The BMS TGFβR inhibitor prodrug, “ compound 10 ,” demonstrates antitumor efficacy comparable to the parent compound ( BMS-986260 ) in a syngeneic model with once-weekly dosing, while reducing the systemic exposure of BMS-986260. Reducing the systemic exposure of a TGFβR inhibitor is important due to previously observed mechanism-based cardiac [...]
Compound 10: A TGFβR Inhibitor Prodrug
compound 10
tumor specific prodrug of TGFβR inhibitor QW dosing, improved tumor-to-heart ratio BMS-986260 prodrug w/ self-immolative link. Journal of Medicinal Chemistry Bristol Myers Squibb, Princeton, NJ
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