Brilanestrant
{{Drugbox | Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = (2E)-3-{4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl]phenyl}prop-2-enoic acid | image = | width =
| tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = Oral
| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =
| CAS_number_Ref = | CAS_number = 1365888-06-7 | CAS_supplemental = | ATCvet = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 56941241 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 35308225 | UNII = 9MM2R1A06R | KEGG = | ChEBI = | ChEMBL =
| C=26 | H=20 | Cl=1 | F=1 | N=2 | O=2 | molecular_weight = 446.900603 g/mol | smiles = CCC(=C(C1=CC=C(C=C1)C=CC(=O)O)C2=CC3=C(C=C2)NN=C3)C4=C(C=C(C=C4)F)Cl | StdInChI_Ref = | StdInChI = 1S/C26H20ClFN2O2/c1-2-21(22-10-9-20(28)14-23(22)27)26(18-8-11-24-19(13-18)15-29-30-24)17-6-3-16(4-7-17)5-12-25(31)32/h3-15H,2H2,1H3,(H,29,30)(H,31,32)/b12-5+,26-21+ | StdInChIKey_Ref = | StdInChIKey = BURHGPHDEVGCEZ-KJGLQBJMSA-N | synonyms = GDC-0810, ARN-810, RG-6046, RO-7056118 }}
Brilanestrant (INN) (developmental code names GDC-0810, ARN-810, RG-6046, RO-7056118) is a non-steroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was discovered by Aragon Pharmaceuticals and is under development by Genentech for the treatment of locally advanced or metastatic estrogen receptor (ER)-positive breast cancer.[1][2][3][4][5] As of September 2016, it is in phase II clinical trials for this indication.[2][5] Similarly to tamoxifen, a SERM, brilanestrant shows some capacity to activate the ER in certain contexts and possesses weak estrogenic activity in the rat uterus, and unlike fulvestrant, which is currently the only SERD to have been marketed, brilanestrant is not a steroid and is orally bioavailable and does not need to be administered by intramuscular injection.[3][4] Brilanestrant has been found to be active in tamoxifen- and fulvestrant-resistant in vitro models of human breast cancer.[5][6] Side effects observed in clinical studies of brilanestrant thus far have included diarrhea, nausea, and fatigue of mostly mild-to-moderate severity.[5]
See also
References
- ^ http://www.who.int/medicines/publications/druginformation/LP_115.pdf
- ^ a b http://adisinsight.springer.com/drugs/800037835
- ^ a b Lai, Andiliy; Kahraman, Mehmet; Govek, Steven; Nagasawa, Johnny; Bonnefous, Celine; Julien, Jackie; Douglas, Karensa; Sensintaffar, John; Lu, Nhin; Lee, Kyoung-jin; Aparicio, Anna; Kaufman, Josh; Qian, Jing; Shao, Gang; Prudente, Rene; Moon, Michael J.; Joseph, James D.; Darimont, Beatrice; Brigham, Daniel; Grillot, Kate; Heyman, Richard; Rix, Peter J.; Hager, Jeffrey H.; Smith, Nicholas D. (2015). "Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts". Journal of Medicinal Chemistry. 58 (12): 4888–4904. doi:10.1021/acs.jmedchem.5b00054. ISSN 0022-2623.
- ^ a b Joseph, James D; Darimont, Beatrice; Zhou, Wei; Arrazate, Alfonso; Young, Amy; Ingalla, Ellen; Walter, Kimberly; Blake, Robert A; Nonomiya, Jim; Guan, Zhengyu; Kategaya, Lorna; Govek, Steven P; Lai, Andiliy G; Kahraman, Mehmet; Brigham, Dan; Sensintaffar, John; Lu, Nhin; Shao, Gang; Qian, Jing; Grillot, Kate; Moon, Michael; Prudente, Rene; Bischoff, Eric; Lee, Kyoung-Jin; Bonnefous, Celine; Douglas, Karensa L; Julien, Jackaline D; Nagasawa, Johnny Y; Aparicio, Anna; Kaufman, Josh; Haley, Benjamin; Giltnane, Jennifer M; Wertz, Ingrid E; Lackner, Mark R; Nannini, Michelle A; Sampath, Deepak; Schwarz, Luis; Manning, Henry Charles; Tantawy, Mohammed Noor; Arteaga, Carlos L; Heyman, Richard A; Rix, Peter J; Friedman, Lori; Smith, Nicholas D; Metcalfe, Ciara; Hager, Jeffrey H (2016). "The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer". eLife. 5. doi:10.7554/eLife.15828. ISSN 2050-084X.
{{cite journal}}: CS1 maint: unflagged free DOI (link) - ^ a b c d "Evaluating an ER Degrader for Breast Cancer". Cancer Discovery. 5 (7): OF15–OF15. 2015. doi:10.1158/2159-8290.CD-NB2015-068. ISSN 2159-8274. PMID 25956960.
- ^ Govek, Steven P.; Nagasawa, Johnny Y.; Douglas, Karensa L.; Lai, Andiliy G.; Kahraman, Mehmet; Bonnefous, Celine; Aparicio, Anna M.; Darimont, Beatrice D.; Grillot, Katherine L.; Joseph, James D.; Kaufman, Joshua A.; Lee, Kyoung-Jin; Lu, Nhin; Moon, Michael J.; Prudente, Rene Y.; Sensintaffar, John; Rix, Peter J.; Hager, Jeffrey H.; Smith, Nicholas D. (2015). "Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft". Bioorganic & Medicinal Chemistry Letters. 25 (22): 5163–5167. doi:10.1016/j.bmcl.2015.09.074. ISSN 0960-894X.
External links
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