title: Structure, development, preclinical and clinical efficacy of tivozanib (KRN-951, AV-951).
abstract: Tivozanib hydrochloride monohydrate (tivozanib; formerly KRN-951, AV-951) is a potent pan-VEGF receptor tyrosine kinase inhibitor. The biological activity of tivozanib seems to outstand that of other VEGF tyrosine kinase inhibitors. In Phase I studies, observed side effects are generally mild, with hypertension being the most common adverse event. In single-agent Phase II and III studies in patients with advanced or metastatic renal cell carcinoma, tivozanib has demonstrated convincing clinical activity. Further clinical trials of tivozanib combined with various cytotoxic drug regimens as well as other classes of target-specific anticancer agents (e.g., mTOR inhibitors) for other indications are underway. Tivozanib has not yet been approved for regular use.
authors.affiliation: Erasmus University Medical Center & Daniel den Hoed Cancer Center, Department of Medical Oncology, PO Box 2040, 3000 CA Rotterdam, The Netherlands. b.haberkorn@erasmusmc.nl
authors.forename: Brigitte C M
authors.initials: BC
authors.lastname: Haberkorn
authors.forename: Ferry A L M
authors.initials: FA
authors.lastname: Eskens
mesh_terms: D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000627:therapeutic use; D002292:Carcinoma, Renal Cell / Q000188:drug therapy*; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007680:Kidney Neoplasms / Q000188:drug therapy*; D010671:Phenylurea Compounds / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D010671:Phenylurea Compounds; D011804:Quinolines; C553176:tivozanib