Drug Dictionary

carmustine sustained-release implant wafer
A sustained release (SR) implant wafer containing the lipophilic nitrosourea carmustine (BCNU) with antineoplastic activity. Upon intracranial administration of the implant wafer and subsequent release of BCNU from the wafer, this agent alkylates and cross-links DNA during all phases of the cell cycle, resulting in the disruption of DNA function, cell cycle arrest, and apoptosis. This wafer contains the biodegradable copolymer PLGA (poly(lactide-co-glycolide) as the major drug delivery vehicle which is slowly degraded into water and carbon dioxide thereby continuously releasing BCNU over approximately 3-4 weeks. Compared to systemic administration of BCNU alone, this local SR formulation is able to maintain higher drug concentrations locally over a longer period of time while minimizing exposure to other tissues.
carrageenan-containing gel
A water-based, vaginal moisturizing gel containing a mixture of lambda- and kappa- carrageenans, sulfated polysaccharides derived from red seaweed (Chondrus crispus), with potential microbicidal activity against various viruses, including human papillomavirus (HPV), human immunodeficiencyvirus (HIV) and human herpes simplex virus (HSV). Upon vaginal insertion via an applicator, carrageenan specifically binds to the viral capsids, which prevents the binding of virions to heparan sulfate proteoglycan (HSPG) receptors or other, as of yet not fully identified, cellular proteins. In addition, the viral binding of carrageenan may also interfere with conformational changes within the virions after cellular attachment. This inhibits viral infection. Certain HPV types cause cervical cancer; therefore, the prevention of HPV infection by this gel may subsequently prevent the development of cervical cancer.
carrot/Ji-Lin ginseng/licorice root/tangerine peel soy beverage
A soy-based powdered nutritional supplement drink containing carrot, Jilin ginseng, licorice root and tangerine peel with potential antioxidant, immunomodulating and protective activities. Besides vitamin C, E and other phytochemicals, carrot/Jilin ginseng/licorice root/tangerine peel/soy beverage contains a high amount of soy protein. This beverage may have a beneficial effect on overall nutrition and the immune system.
Cartilade
(Other name for: shark cartilage)
carubicin
An anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis.
carvedilol
A synthetic antihypertensive methoxyphenoxy- 2-propanol derivative with no intrinsic sympathomimetic activity, Carvedilol acts as a nonselective beta-adrenoceptor blocking agent (S(-) enantiomer) and as an alpha 1-adrenoceptor blocker (R(+) and S(-) enantiomers). Its acts more strongly on beta-receptors than on alpha 1-receptors, reduces peripheral vascular resistance by vasodilation, and prevents reflex tachycardia (beta-blockade) so that heart rate is either unchanged or decreased. Carvedilol also reduces renin release through beta-blockade.
carvedilol phosphate extended-release capsule
An extended-release capsule formulation containing the phosphate salt of carvedilol, a nonselective beta-adrenergic blocking agent with alpha 1-adrenergic blocking activity. Carvedilol is a racemic mixture; the S(-) enantiomer non-selectively binds to and blocks beta-adrenergic receptors, exerting negative inotropic and chronotropic effects, leading to a reduction in cardiac output. Both R(+) and S(-) enantiomers bind to and block alpha 1-adrenergic receptors with equal potency, causing vasodilation and a reduction in peripheral vascular resistance. This agent has no intrinsic sympathomimetic activity.
caseinate protein isolate
An isolate comprised of the sodium or calcium salt of the glycoprotein casein, the primary protein found in milk and other dairy products, with anti-catabolic activity.
Casodex
(Other name for: bicalutamide)
casopitant mesylate
The mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. Casopitant competitively binds to and blocks the activity of the NK1 receptor, thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in antiemetic effects. SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK1 receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema.
cathepsin-activatable Cy5 fluorescent imaging probe LUM015
A cathepsin-activatable fluorescent probe with imaging activity. The cathepsin-activatable fluorescent probe LUM015 contains the Cy5 fluorophore linked, via a pan-cathepsin protease cleavable peptide, to a fluorescent quencher. Upon injection, the peptide in LUM015 can be cleaved by cathepsins overexpressed by tumor cells, which releases the quencher and activates the fluorophore. Upon imaging, tumor cells expressing cathepsin family proteases can be detected.
cationic liposome-encapsulated paclitaxel
A cationic liposome preparation of paclitaxel with antineoplastic activity. Paclitaxel, the active ingredient in cationic liposome-encapsulated paclitaxel, binds to tubulin and inhibits the disassembly of microtubules, resulting in the inhibition of mitosis and cellular proliferation, and apoptosis. Cationic liposome encapsulation of paclitaxel allows the delivery of high doses of paclitaxel to target tissues while minimizing systemic toxicity. Tumor endothelial cells may preferentialy bind and internalize cationic liposomes.
catumaxomab
A trifunctional bispecific monoclonal antibody with potential antineoplastic activity. Catumaxomab has two antigen-recognition sites: one for human CD3, a T cell surface antigen; and one for human epithelial cell adhesion molecule (EpCAM), a cell surface antigen expressed by a variety of epithelial tumor cells. In addition, the modified Fc portion of this antibody binds Fc receptors on antingen presenting cells (APCs) such as macrophages and dendritic cells (DCs). Catumaxomab brings T cells, EpCAM-expressing epithelial tumor cells and APCs together into tricellular complexes, which may result in a potent cytotoxic T-lymphocyte (CTL) response against EpCAM-expressing epithelial tumor cells. Fc-mediated binding of APCs in the tricellular complex potentiates EpCAM antigen presentation to T cells and the activation of anti-tumor cytotoxic T cell functions.
Caverject
(Other name for: alprostadil)
CB10-277
A synthetic derivative of dimethylphenyl-triazene related to dacarbazine, with antineoplastic properties. Related to the agent dacarbazine, CB10-277 is converted in vivo to a monomethyl triazene form that alkylates DNA, resulting in inhibition of DNA replication and repair; in addition, this agent may act as a purine analogue, resulting in inhibition of DNA synthesis, and may interact with protein sulfhydryl groups.
CBP/beta-catenin antagonist PRI-724
A potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. Wnt signaling pathway inhibitor PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP (the binding protein of the cAMP response element-binding protein CREB); together with other transcription factors beta-catenin/CBP binds to WRE (Wnt-responsive element) and activates transcription of a wide range of target genes of Wnt/beta-catenin signaling. Blocking the interaction of CBP and beta-catenin by this agent prevents gene expression of many proteins necessary for growth, thereby potentially suppressing cancer cell growth. The Wnt/beta-catenin signaling pathway regulates cell morphology, motility, and proliferation; aberrant regulation of this pathway leads to neoplastic proliferation.
CC-401
A second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity. Based on the chemistry of SP600125, another anthrapyrazolone inhibitor of JNK, CC-401 competitively binds the ATP binding site of JNK, resulting in inhibition of the phosphorylation of the N-terminal activation domain of transcription factor c-Jun; decreased transcription activity of c-Jun; and a variety of cellular effects including decreased cellular proliferation.
CCL21-expressing H1944 cell vaccine
A cancer cell vaccine comprised of the allogeneic human lung adenocarcinoma cell line H1944 that has been transduced ex vivo with adenoviral vector encoding human cytokine chemokine C-C motif ligand 21 (CCL21), with potential immunomodulating and antineoplastic activities. Upon administration, CCL21-expressing H1944 cell vaccine expresses the chemokine CCL21, which may induce an antitumoral cytotoxic T-lymphocyte immune response in the tumor microenvironment. CCL21 has been shown to attract antigen presenting cells (APCs), like leukocytes and DCs, and natural killer (NK) cells and their T-cell effectors to induce a cytotoxic immune response. H1944 cells contain tumor-associated antigens (TAAs) overexpressed in non-small cell lung cancer (NSCLC).
CCR2 antagonist PF-04136309
An orally available human chemokine receptor 2 (CCR2) antagonist with potential immunomodulating and antineoplastic activities. Upon oral administration, CCR2 antagonist PF-04136309 specifically binds to CCR2 and prevents binding of the endothelium-derived chemokine ligand CLL2 (monocyte chemoattractant protein-1 or MCP1) to its receptor CCR2, which may result in inhibition of CCR2 activation and signal transduction. This may inhibit inflammatory processes as well as angiogenesis, tumor cell migration, and tumor cell proliferation. The G-protein coupled receptor CCR2 is expressed on the surface of monocytes and macrophages, stimulates the migration and infiltration of these cell types, and plays an important role in inflammation, angiogenesis, and tumor cell migration and proliferation.
CD-expressing Bifidobacterium APS001F
A recombinant anaerobic bacterium, Bifidobacterium longum, encoding the cytosine deaminase (CD) gene with potential antineoplastic adjuvant activity. Upon injection, the CD-expressing bifidobacterium preferentially localizes and grows in the hypoxic environment of the tumor and expresses CD, an enzyme that catalyzes the intracellular conversion of the prodrug flucytosine (5-FC) into the antineoplastic agent 5-fluorouracil (5-FU). Upon administration of 5-FC, and subsequent localized conversion into 5-FU and its cytotoxic active metabolites, the tumor is specifically exposed to cytotoxic agents while the exposure to normal tissues is minimal.
CD105/Yb-1/SOX2/CDH3/MDM2 polypeptide plasmid DNA vaccine
A plasmid DNA vaccine containing the mammalian expression vector pUMVC3 (pNGVL3) encoding epitopes of CD105 (Endoglin), Y-box binding protein 1 (Yb-1), SRY-box 2 (SOX2), cadherin 3 (CDH3), and murine double minute 2 (MDM2) proteins, with potential immunomodulating and antineoplastic activities. Upon intradermal administration of pUMVC3-CD105/Yb-1/SOX2/CDH3/MDM2-epitopes plasmid DNA vaccine, the plasmid transfects cells and the peptides are expressed. This generates a specific memory Th1 (T-helper) cell immune response, stimulates secretion of cytokines by the T cells and leads to a cytotoxic T-lymphocyte (CTL) response against CD105/Yb-1/SOX2/CDH3/MDM2-expressing tumor cells. CD105/Yb-1/SOX2/CDH3/MDM2 proteins are highly immunogenic tumor associated antigens that are overexpressed in breast cancer. Additionally, these antigens are associated with breast cancer stem cells and with epithelial to mesenchymal transformation (EMT).
CD133 antigen peptide-pulsed autologous dendritic cell vaccine
A cell-based cancer vaccine comprised of autologous dendritic cells (DCs) pulsed with human leukocyte antigen (HLA)-A2-restricted peptides derived from the CD133 antigen, with potential antineoplastic activity. Upon intradermal administration, the CD133 antigen peptide-pulsed autologous DC vaccine may stimulate an anti-tumoral cytotoxic T-lymphocyte (CTL) response against CD133-expressing tumor cells, resulting in tumor cell lysis. CD133, a cancer stem cell marker, is expressed on hematopoietic stem and progenitor cells and overexpressed on many types of cancer cells; it is associated with resistance to chemotherapy and increased cancer survival. HLA-A2 is an MHC class I molecule that presents antigenic peptides to CD8+ T-cells. Epitope design that is restricted to those epitopes that bind most efficiently to HLA-A2 may improve antigenic peptide immunogenicity.
CD138CAR-CD137/TCRzeta-expressing T lymphocytes2013-08-07
T-lymphocytes transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) specific for syndecan-1 (CD138) (CART-138 T cells) coupled to the signaling domain of 4-1BB (CD137), and the zeta chain of the T-cell receptor (TCRzeta), with potential immunomodulating and antineoplastic activities. Upon transfusion, CD138CAR- CD137/TCRzeta -expressing T lymphocytes direct the T-lymphocytes to syndecan-1-expressing tumor cells and induces selective toxicity in those tumor cells. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of syndecan-1. Syndecan-1, a type 1 transmembrane proteoglycan and tumor associated antigen, is overexpressed in a variety of cancer cells. It plays a key role in the regulation of cell growth, differentiation, and adhesion, and its expression is correlated with poor prognosis.
CD19CAR-CD28zeta-4-1BB-expressing allogeneic T lymphocytes
Allogeneic T-lymphocytes transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) coupled to the costimulatory signaling domain CD28, the signaling domain of 4-1BB (CD137), and the zeta chain of the T-cell receptor (TCR), with potential immunomodulating and antineoplastic activities. Upon transfusion, CD19CAR-CD28 zeta-4-1BB-expressing allogeneic T lymphocytes directs the T-lymphocytes to and induces selective toxicity in CD19-expressing tumor cells. CD28, a T-cell surface-associated co-stimulatory molecule, is required for T-cell activation, proliferation, and survival. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19. Furthermore, inclusion of the 4-1BB signaling domain may increase the antitumor activity compared to the inclusion of the CD28 costimulatory domain and TCR zeta chain alone. CD19 antigen is a B-cell specific cell surface antigen, which is expressed in all B-cell lineage malignancies.
CD19CAR-CD3zeta-4-1BB-CD28-expressing autologous T lymphocytes
Autologous T-lymphocytes transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) coupled to three co-stimulatory signaling domains derived from CD28, 4-1BB (CD137), and the zeta chain of the T-cell receptor (TCR)/CD3 complex (CD3-zeta), with potential immunomodulating and antineoplastic activities. Upon transfusion, the CD19CAR-CD3zeta-4-1BB-CD28-expressing autologous T-lymphocytes direct the T-lymphocytes to CD19-expressing tumor cells and induce their selective toxicity. CD28, a T-cell surface-associated co-stimulatory molecule, is required for T-cell activation, proliferation, and survival. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19. CD3-zeta is a transmembrane signaling adaptor polypeptide that regulates the assembly of TCR complexes, modulates the expression of the complex on the cell surface and plays a key role in antigen recognition. CD19 antigen, a B-cell specific cell surface antigen, is expressed in all B-cell lineage malignancies.
CD19CAR-CD3zeta-4-1BB-expressing allogeneic T lymphocytes
Allogeneic T-lymphocytes transduced with a modified lentiviral vector expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) and the zeta chain of the TCR/CD3 complex (CD3-zeta), coupled to the signaling domain of 4-1BB (CD137), with potential immunomodulating and antineoplastic activities. Upon transfusion, CD19CAR-CD3zeta-4-1BB-expressing allogeneic T-lymphocytes direct the T-lymphocytes to CD19-expressing tumor cells, thereby inducing a selective toxicity in CD19-expressing tumor cells. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19 and the inclusion of this signaling domain may increase the antitumor activity compared to the inclusion of the CD3-zeta chain alone. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies.
CD19CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes
Autologous T-lymphocytes transduced with a modified lentiviral vector expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) and the zeta chain of the TCR/CD3 complex (CD3-zeta), coupled to the signaling domain of 4-1BB (CD137), with potential immunomodulating and antineoplastic activities. Upon transfusion, CD19CAR-CD3zeta-4-1BB-expressing autologous T-lymphocytes direct the T-lymphocytes to CD19-expressing tumor cells, thereby inducing a selective toxicity in CD19-expressing tumor cells. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19 and the inclusion of this signaling domain may increase the antitumor activity compared to the inclusion of the CD3-zeta chain alone. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3-zeta (or CD247) is a transmembrane signaling adaptor polypeptide that regulates the assembly of complete TCR complexes and their expression on the cell surface.
CD19CAR-CD3zeta-expressing autologous T lymphocytes
Autologous T-lymphocytes transduced with a modified lentiviral vector expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) and the zeta chain of the TCR/CD3 complex (CD3-zeta), with potential immunomodulating and antineoplastic activities. Upon transfusion, CD19CAR-CD3zeta-expressing autologous T-lymphocytes are directed to CD19-expressing tumor cells, thereby inducing a selective toxicity only in these tumor cells. The CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3-zeta (or CD247) is a transmembrane signaling adaptor polypeptide that regulates the assembly of complete T-cell receptor complexes and their expression on the cell surface.
CD20-targeted polypeptide TRU-015
A proprietary antibody-based single-chain polypeptide with B cell-depleting activity. Significantly smaller than a whole antibody, CD20-targeted polypeptide TRU-015 binds specifically to the B cell-specific cell surface antigen CD20 with full immunoglobulin Fv fragment-type target binding activity and full immunoglobulin Fc fragment-type effector function. This agent transiently depletes CD20-bearing B cells by inducing B cell -directed complement dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC) and B cell apoptosis.
CD3/CD28 costimulated vaccine-primed autologous T-cells
A population of T cells that have been sensitized to vaccine tumor antigen(s) in vivo; collected from the patient; co-stimulated with antibodies to the T-cell cell surface proteins CD3 and CD28 and expanded ex vivo; and then infused into the same patient. CD3, part of the T cell receptor complex, and CD28, a T-cell surface-associated co-stimulatory molecule, are both required for full T-cell activation. Adoptive transfer of CD3/CD28 costimulated vaccine-primed autologous T-cells may induce the production of interferon-gamma (IFN-gamma) and granulocyte-macrophage colony-stimulating factor (GM-CSF) and associated antitumor effects and a graft-versus-tumor (GVT) response.
CD33CAR-CD3zeta-4-1BB-expressing autologous T-lymphocytes
Autologous T-lymphocytes transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) consisting of an anti-CD33 scFv (single chain variable fragment) coupled to the signaling domain of 4-1BB (CD137) and the zeta chain of the T-cell receptor (TCRzeta), with potential immunomodulating and antineoplastic activities. Upon transfusion, CD33-specific CAR retroviral vector-transduced autologous T lymphocytes target CD33-expressing tumor cells and induce selective toxicity in CD33-expressing tumor cells. Following binding to CD33, the 4-1BB co-stimulatory molecule signaling domain enhances both activation and signaling. Inclusion of the 4-1BB signaling domain may also increase the antitumor activity when compared to the inclusion of the CD3-zeta chain alone. CD33 is expressed on normal non-pluripotent hematopoietic stem cells as well as on myeloid leukemia cells.
CD34/TK75-transduced donor lymphocytes
A preparation of donor T-lymphocytes that are transfected with a retroviral vector encoding a chimeric suicide gene consisting of the extracellular and transmembrane domains of human CD34 and mutant 75 of the herpes simplex virus thymidine kinase (HSV-TK75) with potential controllable immunomodulating activity. Donor T cell therapy following allogeneic hematopoietic stem cell (HSC) transplantation may result in a graft-versus-leukemia (GVL) and help control transplant-related viral infections. In the event that graft-versus-host disease (GVHD) develops due to donor lymphocyte infusion, CD34/TK75-transduced donor lymphocytes may be selectively eliminated by administration of the prodrug antiviral agent ganciclovir GCV. In CD34/T75-transduced donor lymphocytes, GCV is phosphorylated by expressed HSV-TK75 to its monophosphate form and, subsequently, converted into its active triphosphate form, which specifically kills the donor lymphocytes. The expressed CD34 moiety of the chimeric suicide gene serves as a selection marker; mutant 75 of HSV-TK confers increased GCV sensitivity.
CD4+CD25+ regulatory T cells
Regulatory T cells that express CD4 and CD25 (interleukin 2 receptor) antigens, with immunomodulating activity.. CD4+CD25+ T regulatory cells (Tregs), a subset of CD4+ T cells expressing high levels of CD25 and the transcription factor Foxp3, are essential in maintaining immunologic homeostasis, preventing autoimmunity by suppressing self-reactive T cells; CD4+CD25+ Tregs may induce tolerance to allogeneic organ transplants such as hematopoetic stem cell transplants (HSCTs).
CD40 agonist monoclonal antibody CP-870,893
A fully human monoclonal antibody (mAb) agonist of the cell surface receptor CD40 with potential immunostimulatory and antineoplastic activities. Similar to the CD40 ligand (CD40L or CD154), CD40 agonist monoclonal antibody CP-870,893 binds to CD40 on a variety of immune cell types, triggering the cellular proliferation and activation of antigen-presenting cells (APCs), activating B cells and T cells, and enhancing the immune response; in addition, this agent may activate CD40 present on the surfaces of some solid tumor cells, resulting in apoptosis and decreased tumor growth. CD40, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on various immune cells, many B-cell malignancies, and some solid tumors, mediating both indirect tumor cell killing through the activation of the immune system and direct tumor cell apoptosis.
CD95 ECD/IgG-Fc fusion protein APG101
A human, soluble fusion protein consisting of the extracellular domain of the CD95 receptor fused to the Fc-domain of the human IgG antibody, with potential antineoplastic activity. CD95 ECD/IgG-Fc fusion protein APG101 binds to the CD95 ligand (CD95L) and blocks the binding of CD95L to the CD95 receptor. In tumor cells, blockage of CD95L-mediated signaling pathways may prevent cell migration and invasive cell growth; in healthy cells, blockage of CD95L-mediated signaling pathways may prevent apoptosis and may protect cell damage. Activation of the CD95 receptor plays an important role in the initiation of apoptosis in healthy cells or the invasive growth of cancer cells.
CDA inhibitor E7727/decitabine combination agent ASTX727
An orally available combination agent containing the cytidine deaminase (CDA) inhibitor E7727 and the cytidine antimetabolite decitabine, with potential antineoplastic activity. Upon oral administration of ASTX727, the CDA inhibitor E7727 binds to and inhibits CDA, an enzyme primarily found in the gastrointestinal (GI) tract and liver that catalyzes the deamination of cytidine and cytidine analogs. This prevents the breakdown of decitabine, increasing its bioavailability and efficacy while decreasing GI toxicity due to the administration of lower doses of decitabine. Decitabine exerts its antineoplastic activity through the incorporation of its triphosphate form into DNA, which inhibits DNA methyltransferase and results in hypomethylation of DNA. This interferes with DNA replication and decreases tumor cell growth.
CDC7 kinase inhibitor BMS-863233
An orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. CDC7 kinase inhibitor BMS-863233 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell apoptosis, and the inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells. CDC7, a serine-threonine kinase overexpressed in a variety of tumor cell types, plays an essential role in the initiation of DNA replication by activating origins of replication.
CDC7 kinase inhibitor NMS-1116354
An orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. CDC7 kinase inhibitor NMS-1116354 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell apoptosis, and the inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells. The serine-threonine kinase CDC7 initiates DNA replication by phosphorylating MCM2 (minichromosome maintenance complex component 2) at Ser40 and Ser53.
CDK inhibitor P276-00
A flavone and cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. P276-00 selectively binds to and inhibits Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation.
CDK inhibitor SNS-032
A 2-aminothiazole-derived, small-molecule cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. CDK inhibitor SNS-032 selectively binds to CDKs 2, 7, and 9, preventing their phosphorylation and activation; inhibition of CDK activity may result in cell cycle arrest, the induction of apoptosis and decreased tumor cell proliferation in susceptible tumor cell populations. This agent has been shown to sensitize radioresistant tumor cells to ionizing radiation.
CDK2/TRKA inhibitor PHA-848125 AC
An orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. CDKs are serine/threonine kinases involved in regulation of the cell cycle and may be overexpressed in some cancer cell types. The neurotrophin receptor TRKA is mutated in a variety of cancer cell types.
CDK4 inhibitor P1446A-05
A protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity. CDK4 inhibitor P1446A-05 specifically inhibits CDK4-mediated G1-S phase transition, arresting cell cycling and inhibiting cancer cell growth. The serine/threonine kinase CDK4 is found in a complex with D-type G1 cyclins and is the first kinase to become activated upon mitogenic stimulation, releasing cells from a quiescent stage into the G1/S growth cycling stage; CDK-cyclin complexes have been shown to phosphorylate the retinoblastoma (Rb) transcription factor in early G1, displacing histone deacetylase (HDAC) and blocking transcriptional repression.
CDK4/6 dual inhibitor LY2835219
An orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. CDK4/6 dual inhibitor LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.
CDK4/6 inhibitor LEE011
An orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.
CDKI AT7519
An orally bioavailable small molecule with potential antineoplastic activity. AT7519M selectively binds to and inhibits cyclin dependent kinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are serine/theronine kinases involved in regulation of the cell cycle and may be overexpressed in some types of cancer cells.
CDKI R547
An orally bioavailable diaminopyrimidine cyclin-dependent kinase inhibitor (CDKI) with potential antineoplastic activity. CDKI R547 selectively binds to and inhibits CDKs, especially CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1. The inhibition of CDKs results in cell cycle arrest, inhibition of tumor cell proliferation, and induction of apoptosis. Through CDK inhibition, this agent also reduces phosphorylation of the retinoblastoma (Rb) protein, thus preventing activation of transcription factor E2F and so further suppressing tumor cell proliferation.CDKs are ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and are frequently overexpressed in tumor cells.
CDKs/JAK2/FLT3 inhibitor TG02 citrate
An orally bioavailable citrate salt form of TG02, a multi-kinase inhibitor for cyclin dependent kinase (CDK) subtypes 1, 2, 7 and 9, Janus-associated kinase 2 (JAK2), FMS-related tyrosine kinase 3 (FLT3, FLK2, STK1), with potential antineoplastic activity. Upon oral administration, CDK/JAK2/FLT3 Inhibitor TG02 binds to and inhibits the CDK subtypes, JAK2, and FLT3. TG02 also inhibits, to a lesser extent, TYK2, TYRO3, STAT5 and P38delta. This may result in both an induction of apoptosis and an inhibition of tumor cell proliferation in cancer cells that overexpress these kinases. JAK2, often upregulated or mutated in a variety of cancer cells, mediates STAT3 activation and plays a key role in tumor cell proliferation and survival. CDKs are serine/threonine kinases that play key roles in the regulation of the cell cycle and cellular proliferation. FLT3, a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias.
Ce-Vi-Sol
(Other name for: ascorbic acid)
CEA-Scan
(Other name for: arcitumomab)
CEA/tetanus toxoid T helper epitope fusion protein-expressing DNA plasmid vaccine
A plasmid vaccine encoding wild type human carcinoembryonic antigen (CEA) fused to a tetanus toxoid T helper epitope, with potential antineoplastic activity. Upon vaccination and subsequent intradermal electroporation, CEA/tetanus toxoid T helper epitope fusion protein-expressing DNA plasmid vaccine may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells. CEA, a tumor associated antigen, is overexpressed in a variety of cancer cell types. The tetanus toxoid helper peptide epitope, obtained from the bacterial Clostridium tetani toxoid, binds to class II MHC molecules and increases the helper T-cell response thereby inducing an increased and long-term immune response.
CeaVac
(Other name for: monoclonal antibody 3H1 anti-idiotype vaccine)
cebranopadol
An orally available antagonist of the nociceptin receptor opioid receptor like -1 (ORL-1), with potential analgesic activity. Upon oral administration, cebranopadol binds to ORL-1 and prevents its interaction with nociceptin. This leads to a decrease of nociceptin/ORL-1-mediated signaling and interferes with the sensation of pain, which results in an analgesic effect. Nociceptin is a neuropeptide involved in the regulation of pain.
Cecon
(Other name for: ascorbic acid)
CeeNU
(Other name for: lomustine)
cefazolin sodium
The sodium salt of cefazolin, a beta-lactam antibiotic and first-generation cephalosporin with bactericidal activity. Cefazolin binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, which results in the weakening of the bacterial cell wall and cell lysis.
cefepime hydrochloride
The hydrochoride salt of a semi-synthetic, beta-lactamase-resistant, fourth-generation cephalosporin antibiotic derived from an Acremonium fungal species with broad-spectrum bactericidal activity. Administered parenterally, cefipime inhibits bacterial cell wall synthesis by binding to and inactivating penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, resulting in a reduction of bacterial cell wall stability and cell lysis. This agent is more active against a variety of Gram-positive pathogens compared to third-generation cephalosporins.
cefmetazole sodium
The sodium salt of the second-generation, semi-synthetic, beta-lactam cephalosporin cefmetazole with antibacterial activity. Cefmetazole binds to penicillin-binding proteins (PBPs) and prevents the crosslinking of peptidoglycan, which may result in the inhibition of cell wall synthesis, the loss of cell wall integrity, and bacterial cell wall rupture. PBPs are transpeptidases that are responsible for peptidoglycan crosslinking.
cefotaxime
A third generation semisynthetic cephalosporin antibiotic with bactericidal activity. Cefotaxime inhibits mucopeptide synthesis by binding to and inactivating penicillin binding proteins thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of bacterial cell walls. This results in a reduction of cell wall stability and causes cell lysis.
cefpodoxime proxetil
A third generation semi-synthetic cephalosporin and a beta-lactam antibiotic with bactericidal activity. Cefpodoxime's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefpodoxime inhibits bacterial septum and cell wall synthesis formation.
ceftazidime sodium
The sodium salt of ceftazidime, a third-generation cephalosporin antibiotic with bactericidal activity. Ceftazidime binds to and inactivates penicillin-binding proteins (PBPs), enzymes located on the inner membrane of the bacterial cell wall, resulting in the weakening of the bacterial cell wall and cell lysis. Compared to the second and first generation cephalosporins, ceftazidime is more active against gram-negative bacteria and less active against gram-positive bacteria. Ceftazidine also crosses the blood-brain barrier and reaches therapeutic concentrations in the central nervous system (CNS). PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity.
ceftobiprole medocaril
A water-soluble prodrug of ceftobiprole, a pyrrolidinone cephalosporin antibiotic, with bactericidal activity. Ceftobiprole binds to and inactivates penicillin-binding proteins (PBPs), enzymes involved in the terminal stages of bacterial cell wall assembly and cell wall reshaping during bacterial growth and division. This agent exhibits a broad spectrum of activity against gram-negative and gram-positive pathogens including methicillin-resistant S. aureus (MRSA), vancomycin-intermediate S. aureus (VISA) and vancomycin-resistant S. aureus (VRSA). Ceftobiprole is refractory to hydrolysis by class A and class C lactamases.
ceftriaxone sodium
The sodium salt form of ceftriaxone, a beta-lactam, third-generation cephalosporin antibiotic with bactericidal activity. Ceftriaxone binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis. Compared to the second and first generation cephalosporins, ceftriaxone is more active against gram-negative bacteria and less active against gram-positive bacteria. Ceftriaxone also crosses the blood-brain barrier and reaches therapeutic concentrations in the central nervous system (CNS).
Celebrex
(Other name for: celecoxib)
Celestone
(Other name for: betamethasone)
Celiptium
(Other name for: elliptinium acetate)
cell cycle checkpoint/DNA repair antagonist IC83
A proprietary agent with potential antineoplastic activity. Cell cycle checkpoint/DNA repair antagonist IC83 IC83 inhibits cell cycle checkpoint/DNA repair enzymes, which may result in enhanced cytotoxicity of DNA damaging agents and diminished tumor cell resistance to chemotherapy and radiation therapy.Cell cycle checkpoint/DNA repair enzymes are involved in the recognition and repair of damaged DNA and are overexpressed in many types of cancer cells.
cenisertib
An orally bioavailable, synthetic, small-molecule multi-Aurora kinase inhibitor with potential antineoplastic activity. Cenisertib selectively binds to and inhibits multiple Aurora kinases (AKs), which may result in the inhibition of cell division and proliferation, and the induction of apoptosis in tumor cells that overexpress AKs. Overexpressed in certain tumor cell types, AKs, a family of serine-threonine kinases, are important regulators of cell division and proliferation that are involved in controlling chromatid segregation.
Cenolate
(Other name for: ascorbic acid)
CEOP regimen
A chemotherapy regimen consisting of cyclophosphamide, epirubicin, Oncovin (vincristine), and prednisone which may be used in the treatment of aggressive non-Hodgkin lymphomas. (NCI Thesaurus)
Cerazette
(Other name for: desogestral)
Cereport
(Other name for: lobradimil)
Cerespan
(Other name for: papaverine)
ceritinib
An orally available inhibitor of the receptor tyrosine kinase activity of anaplastic lymphoma kinase (ALK) with antineoplastic activity. Upon administration, ceritinib binds to and inhibits wild-type ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to both the disruption of ALK-mediated signaling and the inhibition of cell growth in ALK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK dysregulation and gene rearrangements are associated with a variety of tumor cell types.
certolizumab
A Fab fragment of a recombinant, humanized monoclonal antibody directed against the proinflammatory cytokine tumor necrosis factor-alpha (TNF-alpha), with anti-inflammatory activity. Upon administration, certolizumab binds to TNF-alpha, preventing the interaction of this cytokine with endogenous cell surface receptors, thereby rendering TNF-alpha inactive and inhibiting TNF-mediated inflammatory responses. TNF-alpha is a protein involved in inflammation, cell survival, and apoptosis.
Cervene
(Other name for: TGFa-PE38 immunotoxin)
cesium Cs 131
An unstable radioisotope of cesium (Cs) with radiocytotoxic application. Cs-131 is a gamma photon-emitting radionuclide with high energy and a relatively short half-life of 9.7 days. When used in prostate brachytherapy, Cs-131 demonstrated advantages over other commonly used isotopes.
cesium Cs 137
A radioactive isotope of cesium with an atomic mass of 139 and potential application in radiotherapy. Cesium Cs 137 is prevalent due to its spontaneous production, which occurs as a result of nuclear fission of other radioactive materials, such as uranium and plutonium. This radionuclide has a relatively long half-life, 30 years, and decays by emitting beta particles. Both Cs 137 and its metastable nuclear isomer, barium-137m, emit gamma radiation of moderate energy and so are used in sterilization procedures in the food industry or in hospital environments.
Cetacort
(Other name for: therapeutic hydrocortisone)
Cetane
(Other name for: ascorbic acid)
cetuximab-IRDye 800
An immunoconjugate comprised of the recombinant chimeric monoclonal antibody cetuximab conjugated to the N-hydroxysuccinamide (NHS) ester form of the near-infrared (NIR) fluorescent dye IRDye 800CW (cetuximab-IRDye 800) with potential imaging use. The antibody moiety of cetuximab-IRDye 800 binds to the extracellular domain of the epidermal growth factor receptor (EGFR). Upon binding, IRDye 800 may be detected using NIR imaging, which facilitates the visualization and quantification of EGFR-expressing tumor cells. EGFR is a receptor tyrosine kinase that may be overexpressed on the cell surfaces of various tumor types.
Cevalin
(Other name for: ascorbic acid)
cFMS tyrosine kinase inhibitor ARRY-382
A small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; cFMS) with potential antineoplastic activity. cFMS tyrosine kinase inhibitor ARRY-382 binds to and inhibits the activity of cFMS. By preventing colony-stimulating factor-1 (CSF-1)-cFMS signaling, this agent may inhibit tumor cell proliferation in cFMS-overexpressing tumor cells. cFMS, a tyrosine kinase receptor, is overexpressed in certain tumor cell types and plays an essential role in macrophage differentiation and regulation of cell proliferation.
checkpoint kinase 1 inhibitor LY2606368
An inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity. Upon administration, LY2606368 selectively binds to chk1, thereby preventing activity of chk1 and abrogating the repair of damaged DNA. This may lead to an accumulation of damaged DNA and may promote genomic instability and apoptosis. LY2606368 may potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapeutic agents. Chk1, a serine/threonine kinase, mediates cell cycle checkpoint control and is essential for DNA repair and plays a key role in resistance to chemotherapeutic agents.
checkpoint kinase inhibitor AZD7762
A synthetic small molecule inhibitor of checkpoint kinases (Chks) with potential chemosensitizing activity. AZD7762 binds to and inhibits Chks, which may prevent cell cycle arrest and subsequent nucleotide excision repair in DNA-damaged tumor cells, resulting in tumor cell apoptosis. This agent may enhance the cytotoxicity of DNA-damaging agents. Chks are protein kinases that regulate either G1/S or G2/M transitions in the cell cycle. In the presence of DNA damage or incomplete DNA replication, Chks become activated and initiate cell cycle arrest to allow DNA repair or the completion of DNA replication.
Chemophase
(Other name for: recombinant human hyaluronidase)
chiauranib
An orally available, small molecule inhibitor of select serine-threonine kinases, including aurora kinase B (aurora B), vascular endothelial growth factor receptors (VEGFRs), stem cell factor receptor (c-KIT), and platelet-derived growth factor receptors (PDGFRs), with potential antineoplastic activity. Upon oral administration, chiauranib binds to and inhibits the activity of aurora B, VEGFRs, c-kit and PDGFRs, which may result in a decrease in the proliferation of tumor cells that overexpress these kinases. These kinases are overexpressed by a variety of cancer cell types.
chidamide
An orally bioavailable benzamide type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Chidamide selectively binds to and inhibits HDAC leading to an increase of acetylation levels of histone protein H3. This agent also inhibits the expression of signaling kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, a class of enzymes that deacetylate chromatin histone proteins, are upregulated in many tumor types and play key roles in gene expression. Compared to some other benzamide type HDAC inhibitors, chidamide is more stable, more resistant to degradation and has a longer half-life.
chimeric Ad11p/Ad3 oncolytic virus
A complex, replication-selective, E1B and partial E3 gene deleted, adenovirus type 11p (Ad11p)/Ad3 chimeric oncolytic virus with potential antineoplastic activity. Upon intralesional injection of chimeric Ad11p/Ad3 oncolytic virus, the adenovirus selectively and rapidly replicates in cancer cells; however, it is unable to replicate in normal, healthy cells. This induces a selective adenovirus-mediated cytotoxicity in cancer cells, which leads to cancer cell lysis. Following the lysis of infected cells, the replicated virus is released and can infect adjacent cells, which both induces further tumor cell oncolysis and may activate the immune system to kill the infected tumor cells. The E1B protein causes p53 inactivation in host cells, which promotes viral replication. Deletion of E1B prevents replication in normal, healthy cells that express wild-type p53. The mutation and subsequent inactivation of p53 in cancer cells enables the E1B-deleted adenovirus to selectively replicate in cancer cells. Partial deletion of the E3 gene, which encodes the adenovirus death protein, enhances the safety profile of the administered adenovirus.
Chinese herbal formulation PHY906
An oral traditional Chinese herbal formulation in powder form containing a spray dried aqueous extract from the herbs Scutellaria baicalensis, Glycyrrhiza uralensis, Ziziphus jujuba and Paeonia lactiflora with potential immunomodulating and chemoprotective activities. Although the mechanism of actions remain to be fully elucidated, PHY906 possesses a wide range of pharmacological activities such as the enhancement of oral uptake of pharmacologically active agents, inhibition of CYP3A4, modulation of certain cytokines, macrophages and lymphocytes, and inhibition of expression of MMP, NF-kB, beta-glucuronidase, the NK-1 receptor, and the delta-opioid receptor.
Chinese herbs
Herbs used in Chinese Herbal Therapy for toxicity attenuation.
chk1 inhibitor PF-477736
A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity. Chk1 inhibitor PF-477736 inhibits chk1, an ATP-dependent serine-threonine kinase that is a key component in the DNA replication-monitoring S/G2 checkpoint system. By overriding the last checkpoint defense against DNA damaging agent-induced lethal damage, chk1 inhibitor PF-477736 may potentiate the antitumor efficacy of various chemotherapeutic agents against tumor cells with intrinsic checkpoint defects.
Chk1 inhibitor SCH 900776
An agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. Chk1 inhibitor SCH 900776 specifically binds to and inhibits Chk1, which may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases to undergo DNA repair prior to entry into mitosis; tumor cells may thus be sensitized to the DNA-damaging effects of ionizing radiation and alkylating chemotherapeutic agents. Chk1 is an ATP-dependent serine-threonine kinase that in response to DNA damage phosphorylates cdc25 phosphatases, resulting in inhibitory tyrosine phosphorylation of CDK-cyclin complexes and cell cycle arrest.
chlorambucil-prednisone regimen
A chemotherapy regimen consisting of chlorambucil and prednisone used for the treatment of chronic lymphocytic leukemia. (NCI Thesaurus)
chlorhexidine
A biguanide compound used as an antiseptic agent with topical antibacterial activity. Chlorhexidine is positively charged and reacts with the negatively charged microbial cell surface, thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine penetrates into the cell and causes leakage of intracellular components leading to cell death. Since gram positive bacteria are more negatively charged, they are more sensitive to this agent.
chlorhexidine gluconate
The gluconate salt form of chlorhexidine, a biguanide compound used as an antiseptic agent with topical antibacterial activity. Chlorhexidine gluconate is positively charged and reacts with the negatively charged microbial cell surface, thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine gluconate penetrates into the cell and causes leakage of intracellular components leading to cell death. Since gram positive bacteria are more negatively charged, they are more sensitive to this agent.
chlorogenic acid
A polyphenol and the ester of caffeic acid and quinic acid that is found in coffee and black tea, with potential antioxidant and chemopreventive activities. Chlorogenic acid scavenges free radicals, which inhibits DNA damage and may protect against the induction of carcinogenesis. In addition, this agent may upregulate the expression of genes involved in the activation of the immune system and enhance activation and proliferation of cytotoxic T-lymphocytes, macrophages, and natural killer cells. Chlorogenic acid also inhibits the activity of matrix metalloproteinases.
chloroquine
A 4-aminoquinoline with antimalarial, anti-inflammatory, and potential chemosensitization and radiosensitization activities. Although the mechanism is not well understood, chloroquine is shown to inhibit the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin, thereby resulting in the accumulation of toxic heme within the parasite. This agent may also interfere with the biosynthesis of nucleic acids. Chloroquine's potential chemosensitizing and radiosensitizing activities in cancer may be related to its inhibition of autophagy, a cellular mechanism involving lysosomal degradation that minimizes the production of reactive oxygen species (ROS) related to tumor reoxygenation and tumor exposure to chemotherapeutic agents and radiation.
chlorotoxin-indocyanine green imaging Agent BLZ-100
A tumor-targeting imaging agent composed of the tumor-specific peptide chlorotoxin (CTX), a 36-amino acid neurotoxin found in the venom of the Leiurus quinquestriatus scorpion, linked to the fluorescent dye indocyanine green (ICG), with potential tumor imaging activity using a near-infrared (NIR) imaging system. Upon intravenous administration of BLZ-100, the CTX moiety of BLZ-100 specifically binds to and is internalized by cancer cells of neuroectodermal origin. Using a NIR imaging system, the ICG, which emits light in the NIR range, permits the intraoperative visualization of tumor cells. This leads to the clear distinction of healthy tissues from tumor cells, and facilitates the surgical removal of tumor tissue while sparing normal, healthy cells.
chlorozotocin
A glucose-linked chloroethylnitrosourea with potential antineoplastic activity. Chlorozotocin alkylates DNA and proteins, induces the formation of interstrand DNA and DNA-protein crosslinks, and causes DNA strand breakage, thereby damaging DNA and resulting in cell death. This agent has been shown to exhibit antitumor and immunomodulatory effects in cell lines and animal models. Chlorozotocin is a mutagen and is less myelotoxic than other nitrosoureas.
chlorpromazine
A phenothiazine and traditional antipsychotic agent with anti-emetic activity. Chlorpromazine exerts its antipsychotic effect by blocking postsynaptic dopamine receptors in cortical and limbic areas of the brain, thereby preventing the excess of dopamine in the brain. This leads to a reduction in psychotic symptoms, such as hallucinations and delusions. Chlorpromazine appears to exert its anti-emetic activity by blocking the dopamine receptors in the chemical trigger zone (CTZ) in the brain, thereby relieving nausea and vomiting.
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