BMS690514 / BMS - LARVOL DELTA

Drug repurposing to identify nilotinib and BMS-690514 as potential SARS-CoV-2 main protease inhibitors: An insight from computational and In vitro study (ACS-Sp 2022) - "Nilotinib, Bemcentinib, and BMS-690514 had EC50 values of 1.1, 2.6, and 32.8 µM, respectively. In conclusion, the results of our computer-aided drug design provide a pathway for rational Mpro inhibitor drug design and the development of COVID-19 antiviral treatments.Fig 1. Molecular modeling guided screening and in vitro evaluation of potential SARS-CoV-2 Mpro inhibitors"

Preclinical • Infectious Disease • Novel Coronavirus Disease • Pneumonia • Respiratory Diseases

Dual HER/VEGF receptor targeting inhibits in vivo ovarian cancer tumor growth (Mol Cancer Ther) - PMID: 24130056; "...ovarian cancer xenografts grown intraperitoneally in athymic nude mice were tested in response to AC480 (pan HER inhibitor, "HERi"), cediranib (pan VEGFR inhibitor "VEGFRi"), or BMS-690514 (combined HER/VEGFR inhibitor "EVRi"). EVRi was superior to both HERi and VEGFRi in terms of tumor growth, final tumor weight and progression-free survival."

Preclinical • Oncology • Ovarian Cancer

Inhibitory effect of ketoconazole on the pharmacokinetics of a multireceptor tyrosine kinase inhibitor BMS-690514 in healthy participants: Assessing the mechanism of the interaction with physiologically-based pharmacokinetic simulations (J Clin Pharmacol) - P=NA, N=17; PMID: 23436267; "The AUC(∞) of 100 mg BMS-690514 concomitantly administered with ketoconazole was similar to that of 200 mg BMS-690514 alone. The dose-normalized C(max) and AUC(∞) of BMS-690514 from the 100-mg BMS-690514/400-mg ketoconazole treatment increased by 55% and 127%, respectively, relative to those from 200 mg BMS-690514 alone."

PK/PD data • Oncology

A phase I trial to determine the safety, pharmacokinetics, and pharmacodynamics of intercalated BMS-690514 with paclitaxel/carboplatin (PC) in advanced or metastatic solid malignancies (Cancer Chemother Pharmacol) - P1, N=34; Sponsor: BMS; NCT00420186; PMID: 23468081; “The MTD was reached at 150 mg/day… Of the 32 patients evaluable for efficacy, there were 12 partial responses including five patients with non-small-cell lung cancer and 12 patients with stable disease.”

P1 data • Oncology

A phase I study of BMS-690514 in Japanese patients with advanced or metastatic solid tumors (Cancer Chemother Pharmacol) - P1, N=9; NCT00516451; BMS-690514 at the dose of 100 mg (N=3) or 200 mg (N=3) was administered once daily to totally nine pts and was well tolerated up to 200 mg; No treatment-related SAEs or DLTs were reported; Five pts had SD

P1 data • Oncology