{{cs1 config |name-list-style=vanc |display-authors=6}} {{Infobox drug | image = Olomorasib.svg | image_class = skin-invert-image | width = 300
<!-- Clinical data --> | tradename = | pregnancy_category = | routes_of_administration = | class = | ATC_prefix = | ATC_suffix = | ATC_supplemental =
<!-- Legal status --> | legal_status =
<!-- Pharmacokinetic data --> | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action = | excretion =
<!-- Identifiers --> | CAS_number = 2649788-46-3 | CAS_supplemental = | PubChem = 156472638 | IUPHAR_ligand = | DrugBank = | ChemSpiderID = 115009373 | UNII = C2VJ83PSN7 | KEGG = D12853 | ChEMBL = | synonyms = LY3537982
<!-- Chemical and physical data --> | IUPAC_name = (4''M'')-2-amino-4-[(4a''S'')-8-chloro-10-fluoro-12-oxo-3-(prop-2-enoyl)-2,3,4,4a,5,6-hexahydro-1''H'',12''H''-pyrazino[2,1-''d''][1,5]benzoxazocin-9-yl]-7-fluoro-1-benzothiophene-3-carbonitrile | C = 25 | H = 19 | Cl = 1 | F = 2 | N = 4 | O = 3 | S = 1 | SMILES = C=CC(=O)N1CCN2[C@H](C1)CCOC3=C(C(=C(C=C3C2=O)F)C4=C5C(=C(SC5=C(C=C4)F)N)C#N)Cl | StdInChI = 1S/C25H19ClF2N4O3S/c1-2-18(33)31-6-7-32-12(11-31)5-8-35-22-14(25(32)34)9-17(28)20(21(22)26)13-3-4-16(27)23-19(13)15(10-29)24(30)36-23/h2-4,9,12H,1,5-8,11,30H2/t12-/m0/s1 | StdInChIKey = OZUPICRWMLEFCS-LBPRGKRZSA-N }}
'''Olomorasib''' ('''LY3537982''') is an experimental anticancer drug which acts as an inhibitor of the G12C mutant form of Kirsten rat sarcoma virus (KRAS), an oncogene commonly present in several forms of cancer. It is in early stage clinical trials against lung and colorectal cancers and advanced solid tumors.<ref>{{cite journal | vauthors = Peng SB, Si C, Zhang Y, Van Horn RD, Lin X, Gong X, Huber L, Donoho G, Curtis C, Strelow JM, Bocchinfuso WP | title = Preclinical characterization of LY3537982, a novel, highly selective and potent KRAS-G12C inhibitor. | journal = Cancer Research | date= July 2021 | volume = 81 | issue = 13_Supplement | pages = 1259 | doi = 10.1158/1538-7445.AM2021-1259 }}</ref><ref name="pmid39175850">{{cite journal | vauthors = Miyashita H, Hong DS | title = Combining EGFR and KRAS G12C Inhibitors for KRAS G12C Mutated Advanced Colorectal Cancer | journal = Journal of Cancer Immunology | volume = 6 | issue = 2 | pages = 62–69 | date = 2024 | pmid = 39175850 | pmc = 11340593 | doi = 10.33696/cancerimmunol.6.086 | url = }}</ref><ref>{{cite journal | doi = 10.1200/JCO.2024.42.3_suppl.94| title = Efficacy and safety of LY3537982, a potent and highly selective KRAS G12C inhibitor in KRAS G12C-mutant GI cancers: Results from a phase 1 study| date = 2024| journal = Journal of Clinical Oncology| volume = 42| issue = 3_suppl| page = 94| vauthors = Hollebecque A, Kuboki Y, Murciano-Goroff YR, Yaeger R, Cassier PA, Heist RS, Fujiwara Y, Deming DA, Ammakkanavar N, Patnaik A, Shimizu T, Call J, Han S, Fink AA, Chen A, Willard MD, Balar AV, Koyama T }}</ref><ref>{{cite journal | doi = 10.1200/JCO.2024.42.16_suppl.8510 | title = Efficacy and safety of olomorasib (LY3537982), a second-generation KRAS G12C inhibitor (G12Ci), in combination with pembrolizumab in patients with ''KRAS'' G12C-mutant advanced NSCLC | date = 2024 | journal = Journal of Clinical Oncology | volume = 42 | issue = 16_suppl | page = 8510 | vauthors = Burns TF, Dragnev KH, Fujiwara Y, Murciano-Goroff YR, Lee DH, Hollebecque A, Koyama T, Cassier PA, Italiano A, Heist RS, Han J, Deming DA, Spira AI, Sabari JK, Chisamore MJ, Fink AA, Chen A, Willard MD, Oxnard GR, Ammakkanavar NR }}</ref><ref>{{cite journal | doi = 10.1200/JCO.2024.42.16_suppl.3007 | title = Pan-tumor activity of olomorasib (LY3537982), a second-generation KRAS G12C inhibitor (G12Ci), in patients with ''KRAS'' G12C-mutant advanced solid tumors | date = 2024 | journal = Journal of Clinical Oncology | volume = 42 | issue = 16_suppl | page = 3007 | vauthors = Heist RS, Koyama T, Murciano-Goroff YR, Hollebecque A, Cassier PA, Han J, Tosi D, Sacher AG, Burns TF, Spira AI, Gomez-Roca CA, Shimizu T, Ammakkanavar NR, Sabari JK, Nagasaka M, Fink AA, Chen A, Willard MD, Oxnard GR, Kuboki Y }}</ref>
== See also == * ACBI3 * Adagrasib * Divarasib * MRTX1133 * Zoldonrasib * Sotorasib
== References == {{reflist}}
Category:Experimental cancer drugs Category:Benzothiophenes Category:Pyrazines Category:Oxazocines Category:Nitriles Category:Fluoroarenes Category:Chloroarenes Category:Amines Category:Carboxamides Category:Cyclic ketones