| 词条 | Larotrectinib |
| 释义 |
| drug_name = | INN = | type = | image = Larotrectinib.svg | caption = | pronounce = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | routes_of_administration = | legal_US = | legal_status = | bioavailability = | protein_bound = | metabolism = | excretion = | CAS_number = 1223403-58-4 | class = | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 46188928 | DrugBank = | ChemSpiderID = 44210503 | UNII = PF9462I9HX | KEGG = D11137 | ChEBI = | ChEMBL = 3889654 | StdInChI = 1S/C21H22F2N6O2/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31)/t14-,18+/m0/s1 | StdInChIKey = NYNZQNWKBKUAII-KBXCAEBGSA-N | synonyms = LOXO-101, ARRY-470 | chemical_formula = | C=21 | H=22 | Ag= | Al= | As= | Au= | B= | Bi= | Br= | Ca= | Cl= | Co= | F=2 | Fe= | Gd= | I= | K= | Li= | Mg= | Mn= | N=6 | Na= | O=2 | P= | Pt= | S= | Sb= | Se= | Sr= | Tc= | Zn= | charge= | molecular_weight = 428.444 g/mol | SMILES =O[C@H]1CCN(C1)C(=O)Nc2cnn3ccc(nc23)N4CCC[C@@H]4c5cc(F)ccc5F | IUPAC_name = (3S)-N5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl3-hydroxypyrrolidine-1-carboxamide }} Larotrectinib (tradename Vitrakvi) is a drug for the treatment of cancer.[1] It is an inhibitor of tropomyosin kinase receptors TrkA, TrkB, and TrkC. It was discovered by Array BioPharma and licensed to Loxo Oncology in 2013. Larotrectinib was initially awarded orphan drug status in 2015 for soft tissue sarcoma, and breakthrough therapy designation in 2016 for the treatment of metastatic solid tumors with NTRK fusion.[2] Some clinical trial results were announced in 2017.[3] On 26 November 2018, Larotrectinib was approved by the FDA[4]. Larotrectinib was the first drug to be specifically developed and approved to treat any cancer containing certain mutations, as opposed to cancers of specific tissues (i.e., the approval is "tissue agnostic"). Several earlier drugs, including pembrolizumab, were eventually approved by the FDA for treatment of specific mutations independent of the type of cancer, but those drugs had been initially developed for specific cancer types.[5] Phase II clinical trials evaluating the drug for efficacy and safety in treating several types of solid tumors are ongoing.[6] See also
References1. ^{{Cite web|url=https://searchusan.ama-assn.org/usan/documentDownload?uri=%2Funstructured%2Fbinary%2Fusan%2Flarotrectnib.pdf|title=STATEMENT ON A NONPROPRIETARY NAME ADOPTED BY THE USAN COUNCIL|last=|first=|date=October 26, 2016|website=ama-assn.org|archive-url=|archive-date=|dead-url=|access-date=}} 2. ^{{cite web|title=Larotrectinib|url=http://adisinsight.springer.com/drugs/800040495|website=AdisInsight|accessdate=31 January 2017}} 3. ^Novel Agent Shows Antitumor Activity in TRK-Fusion Cancers. June 2017 4. ^{{cite web|title=FDA approves larotrectinib for solid tumors with NTRK gene fusions|url=https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm626720.htm|date=November 26, 2018|website=www.fda.gov}} 5. ^{{cite news |last=Dun|first=Lauren|date=27 Nov 2018|title=FDA approves a new cancer drug targeted to genetic mutation, not cancer type|url=https://www.nbcnews.com/health/health-news/fda-approves-new-cancer-drug-targeted-genetic-mutation-not-cancer-n940656|work=NBC|access-date=3 Dec 2018}} 6. ^[https://clinicaltrials.gov/ct2/show/NCT02576431 Study of LOXO-101 (Larotrectinib) in Subjects With NTRK Fusion Positive Solid Tumors (NAVIGATE)] External links
4 : Experimental cancer drugs|Tissue agnostic antineoplastic agents|Eli Lilly and Company|Bayer AG |
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