Monoclonal antibody | |
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Type | Whole antibody |
Source | Chimeric/humanized hybrid (mouse/human) |
Target | TEM1 |
Clinical data | |
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Chemical and physical data | |
Formula | C6532H10050N1726O2054S44 |
Molar mass | 147.0 kg/mol |
Ontuxizumab [1] is a humanized rabbit monoclonal antibody [2] designed for the treatment of cancer. It binds to endosialin (TEM1 or CD248). [3]
Phase I trials are complete and the drug was granted orphan drug status by the FDA for sarcoma. It is currently in phase II trials for melanoma, colorectal cancer, sarcoma, and lymphoma. [4]
An orphan drug is a pharmaceutical agent developed to treat medical conditions which, because they are so rare, would not be profitable to produce without government assistance. The conditions are referred to as orphan diseases.
This drug was developed by Morphotek and Ludwig Institute for Cancer Research. [5]
Lumiliximab is an IgG1k monoclonal antibody that targets CD23. It acts as an immunomodulator and was awarded orphan drug status and fast track designation by the FDA.
Telapristone (INN), as telapristone acetate, is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros Therapeutics for the treatment of breast cancer, endometriosis, and uterine fibroids. It was originally developed by the National Institutes of Health (NIH), and, as of 2017, is in phase II clinical trials for the aforementioned indications. In addition to its activity as an SPRM, the drug also has some antiglucocorticoid activity.
Cixutumumab (IMC-A12) is a human monoclonal antibody for the treatment of solid tumors.
Robatumumab, also known as SCH 717454 and MK-7454 is a monoclonal antibody and an antineoplastic by Merck and Schering-Plough. It binds to CD221, the insulin-like growth factor 1 receptor.
Olaratumab is a monoclonal antibody developed by Eli Lilly and Company for the treatment of solid tumors. It is directed against the platelet-derived growth factor receptor alpha.
Glembatumumab vedotin is an antibody-drug conjugate (ADC) that targets cancer cells expressing transmembrane glycoprotein NMB (GPNMB).
Zoptarelin doxorubicin consists of doxorubicin linked to a small peptide agonist to the luteinizing hormone-releasing hormone (LHRH) receptor. It has been developed as a potential treatment for a number of human cancers. The LHRH receptor is aberrantly present on the cell surface of approximately 80% of endometrial and ovarian cancers, 86% of prostate cancers and about 50% of breast cancers. Whereas in normal tissues, expression of this receptor is mainly confined to the pituitary gland, reproductive organs and hematopoietic stem cells. To a lesser extent the LHRH receptor is also found on the surface of bladder, colorectal, and pancreatic cancers, sarcomas, lymphomas, melanomas, and renal cell carcinomas.
Zibotentan (INN) is an anti-cancer candidate in development by AstraZeneca. It is an endothelin receptor antagonist.
Idoxifene, also known as pyrrolidino-4-iodotamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group which was under development for the treatment of breast cancer and postmenopausal osteoporosis but was never marketed. It reached phase III clinical trials for postmenopausal osteoporosis and phase II clinical trials for breast cancer before development was discontinued in 1999 due insufficient effectiveness in both cases.
Teprotumumab (RG-1507) is an experimental human monoclonal antibody developed by Genmab and Roche. It binds to IGF-1R.
Linsitinib is an experimental drug candidate for the treatment of various types of cancer. It is an inhibitor of the insulin receptor and of the insulin-like growth factor 1 receptor (IGF-1R). This prevents tumor cell proliferation and induces tumor cell apoptosis.
Acolbifene (INN) is a nonsteroidal selective estrogen receptor modulator (SERM) which, as of 2015, is in phase III clinical trials for the treatment of breast cancer.
Depatuxizumab mafodotin (ABT-414) (INN) is an antibody-drug conjugate designed for the treatment of cancer. It is composed of an EGFR IGg1 monoclonal antibody (depatuxizumab) conjugated to the tubulin inhibitor monomethyl auristatin F via a stable maleimidocaproyl link.
Elacestrant (INN) is a nonsteroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was discovered by Eisai and is under development by Radius Health and Takeda for the treatment of menopausal vasomotor symptoms and estrogen receptor (ER)-positive advanced breast cancer, as well as endometrial cancer and kidney cancer. As of September 2016, it is in phase II clinical trials for vasomotor symptoms and breast cancer. Elacestrant has dose-dependent, tissue-selective estrogenic and antiestrogenic activities, with biphasic weak partial agonist activity at the ER at low doses and antagonist activity at higher doses. It shows agonistic activity on bone and antagonistic activity on breast and uterine tissues. Unlike the SERD fulvestrant, elacestrant is able to readily cross the blood-brain-barrier into the central nervous system, where it can target breast cancer metastases in the brain, and is orally bioavailable and does not require intramuscular injection.
Droloxifene, also known as 3-hydroxytamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was developed originally in Germany and later in Japan for the treatment of breast cancer, osteoporosis in men and postmenopausal women, and cardiovascular disorders but was abandoned and never marketed. It reached phase II and phase III clinical trials for these indications before development was discontinued in 2000. The drug was found to be significantly less effective than tamoxifen in the treatment of breast cancer in two phase III clinical trials.
Miproxifene (INN) is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was never marketed. It is a derivative of afimoxifene (4-hydroxytamoxifen) in which an additional 4-isopropyl group is present in the β-phenyl ring. The drug has been found to be 3- to 10-fold more potent than tamoxifen in inhibiting breast cancer cell growth in in vitro models. Miproxifene is the active metabolite of miproxifene phosphate (TAT-59), a phosphate ester and prodrug of miproxifene that was developed to improve its water solubility. Miproxifene phosphate was under development for the treatment of breast cancer and reached phase III clinical trials for this indication but development was discontinued.
Rovalpituzumab tesirine (Rova-T) is an experimental antibody-drug conjugate targeting the protein DLL3 on tumor cells. It was originally developed by Stemcentrx and was purchased by AbbVie. It is being tested for use in small-cell lung cancer.
Pipendoxifene (INN) is a nonsteroidal selective estrogen receptor modulator (SERM) that was under development by Ligand Pharmaceuticals and Wyeth-Ayerst Laboratories for the treatment of breast cancer but was not marketed. It is a member of the 2-phenylindole group of SERMs and is structurally related to zindoxifene and the marketed bazedoxifene. The drug reached phase II clinical trials before its development was discontinued. It was synthesized at the same time as bazedoxifene and was intended as a backup drug for bazedoxifene, only to be developed further if bazedoxifene had failed in clinical trials. No further development was reported after 2002 and it was formally announced that development had been terminated in November 2005.
Onapristone (INN) is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a silent antagonist of the progesterone receptor (PR), in contrast to the related antiprogestogen mifepristone. Moreover, compared to mifepristone, onapristone has reduced antiglucocorticoid activity, shows little antiandrogenic activity, and has 10- to 30-fold greater potency as an antiprogestogen. The medication was under development for clinical use, for instance in the treatment of breast cancer and as an endometrial contraceptive, but was discontinued during phase III clinical trials in 1995 due to findings that liver function abnormalities developed in a majority patients.
Relacorilant is an antiglucocorticoid which is under development by Corcept Therapeutics for the treatment of Cushing's syndrome. It is also under development for the treatment of solid tumors and alcoholism. The drug is a nonsteroidal compound and acts as an antagonist of the glucocorticoid receptor. As of December 2017, it is in phase II clinical trials for Cushing's syndrome and phase I/II clinical studies for solid tumors, while the clinical phase for alcoholism is unknown.
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