A fresh vote against integrins

The disappointment of Vincerx's integrin αvβ3-targeting small-molecule drug conjugate VIP236 has been followed by Novartis dealing this mechanism a fresh blow. The only clinical study of the Swiss group's 177Lu-FF58, a radioconjugate against αvβ3/5, has been terminated, according to clinicaltrials.gov. This is despite the Novartis trial having apparently mandated expression of αvβ3 or αvβ5; notably, Vincerx had declined to set such an inclusion criterion, claiming that αvβ3 was very commonly expressed, before its stock crashed when VIP236 yielded zero responses among 15 patients at last year's AACR conference. In 2017 Novartis bought the readiopharma specialist Advanced Accelerator Applications for $3.9bn, and shortly afterwards it licensed rights to Fujifilm Toyama Chemical's FF-10158, a small-molecule inhibitor of αvβ3/5. 177Lu-FF58 was a lutetium-177-labelled version of FF-10158, and its phase 1 trial started in October 2023, seeking to recruit 116 solid tumour patients. In the event only 24 were enrolled before the study was terminated. "The decision was not based on any safety concerns," clinicaltrials.gov states.

Selected projects against integrin αvβ3

Source: OncologyPipeline.