このADC、構造的な工夫がいくつかあり、Maleimide代替でレトロ反応を抑えたり、SN38と同じ程度の(つまりDXdより低毒性の)Payloadを使ったりしています。Linker部分はTrodelvyと同様のpH応答性のものですね Payloadの毒性が低いから、前述のILDは抑えられている? 2/2 https://t.co/KOcCLDHPzi https://t.co/40lDdS940v
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@JacobPlieth @evaluatevantage Nice summary! MK-2870/SKB-264 payload is not belotecan but a belotecan derivative (named KL610023 or T030)(https://t.co/JoV6eRa2Ko) Also a new TROP2 ADC (FZ-AD004) should enter phase 1 in China soon (https://t.co/VmzDmptZcS
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Preclinical profiles of SKB264, a novel anti-TROP2 antibody conjugated to topoisomerase inhibitor, demonstrated promising antitumor efficacy compared to IMMU-132 https://t.co/c6G9n4SilM https://t.co/PgPOzP6KZa
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Sichuan Kelun’s preclinical development of their Trop-2 TOPO1i ADC (SKB-264 aka MK-2870, after collaboration and licensing agreement with Merck): https://t.co/JoV6eRa2Ko