axitinib axitinib axitinib, sold under the brand name inlyta, is a small molecule tyrosine kinase inhibitor developed by pfizer. it has been shown to significantly inhibit growth of breast cancer in animal (xenograft) models and has shown partial responses in clinical trials with renal cell carcinoma (rcc) and several other tumour types. axitinibclinical datatrade namesinlyta, axinixother namesag013736ahfs/drugs.commonographmedlineplusa612017license data eu ema: by inn us dailymed: axitinib pregnancycategory au: d routes ofadministrationby mouthatc codel01ek01 (who) legal statuslegal status au: s4 (prescription only) ca: ℞-only uk: pom (prescription only) us: ℞-only pharmacokinetic databioavailability58%protein binding>99%metabolismliver (mostly cyp3a4/cyp3a5-mediated but with some contributions from cyp1a2, cyp2c19, ugt1a1)elimination half-life2.5-6.1 hoursexcretionfeces (41%; 12% as unchanged drug), urine (23%)identifiers iupac name n-methyl-2--1h-indazol-6-yl]sulfanyl]benzamide cas number319460-85-0 ypubchem cid6450551iuphar/bps5659drugbankdb06626 ychemspider4953153 yuniic9lvq0yuxgkeggd03218 ychebichebi:66910 nchemblchembl1289926 npdb ligandaxi (pdbe, rcsb pdb)comptox dashboard (epa)dtxsid3049049 echa infocard100.166.384 chemical and physical dataformulac22h18n4osmolar mass386.47 g·mol−13d model (jsmol)interactive image smiles cnc(=o)c1ccccc1sc4ccc3c(c=cc2ccccn2)nc3c4 inchi inchi=1s/c22h18n4os/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14h,1h3,(h,23,27)(h,25,26)/b12-9+ ykey:ritavmqdgbjqjz-fmivxfbmsa-n y ny (what is this?) (verify) it was approved to treat renal cell carcinoma by the u.s. food and drug administration after showing a modest increase in progression-free survival, though there have been reports of fatal adverse effects. approvals and indications renal cell carcinoma it has received approval for use as a treatment for renal cell carcinoma from the us food and drug administration (fda) (27 january 2012), the european medicines agency (ema) (13 september 2012), the uk medicines and healthcare products regulatory agency (mhra) (3 september 2012) and the australian therapeutic goods administration (tga) (26 july 2012). clinical trials a phase ii clinical trial showed good response in combination chemotherapy with gemcitabine for advanced pancreatic cancer. however, pfizer reported on january 30, 2009, that phase iii clinical trials of the drug when used in combination with gemcitabine showed no evidence of improved survival rates over treatments using gemcitabine alone for advanced pancreatic cancer and halted the trial. in 2010, a phase iii trial for previously treated metastatic renal cell carcinoma (mrcc) showed significantly extended progression-free survival when compared to sorafenib. in december 2011, the oncologic drugs advisory committee (odac) voted unanimously to recommend that us fda approve axitinib for the second-line treatment of patients with advanced renal cell carcinoma (rcc), based on the results of the phase iii trial comparing axitinib and sorafenib. it has also been studied in combination with the alk1 inhibitor dalantercept. a study published in 2015 showed that axitinib effectively inhibits a mutated gene (bcr-abl1) that is common in chronic myeloid leukemias and adult acute lymphoblastic leukemias which have become resistant to other tyrosine kinase inhibitors like imatinib. this is one of the first examples of a new indication for an existing drug being discovered by screening known drugs using a patient's own cells. adverse effects