PRT3789 Is a First-in-Human SMARCA2-Selective Degrader That Induces Synthetic Lethality in SMARCA4-Mutated Cancers.

doi:10.1158/0008-5472.CAN-25-1141

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PRT3789 Is a First-in-Human SMARCA2-Selective Degrader That Induces Synthetic Lethality in SMARCA4-Mutated Cancers.

Cancer research - 2 Jan 2026

Hulse Michael, Wang Min, Xu Chaoyi, Carter Jack, Agarwal Anjana, Lu Liang, Pitis Philip, Bhagwat Neha, Rager Joseph, Kurian Justin, Basch Corey, Sivakumar Monisha, Burtell Jessica, Mondal Arpita, Grego Alexander, Moore Andrew, Bachner Carly, Vykuntam Komali, Reichelderfer Anthony, Park Jimin, Cote Joy, Cowart Miles, Osinubi Olusola Peace, Bigot Ludovic, Da Silva Alice, Nobre Catline, Meteau Melissandre, Soares Miguel, Tang Hsin-Yao, Bersch Klare, Dai Chaofeng, Cao Ganfeng, Shen Bo, Emm Tom, Ruepp Stefan, Xavier Jennifer, Tankersley Chris, Heiser Diane, Lee Sang Hyun, Geeganage Sandy, Ruggeri Bruce, Lin Hong, Novotny William, Huang Jane, Vaddi Kris, Combs Andrew, Scherle Peggy, Ito Koichi

Abstract excerpt

SMARCA2 and SMARCA4 are the core catalytic subunits of the switch/sucrose nonfermentable (SWI/SNF) chromatin remodeling complex. Approximately 10% of patients with non-small cell lung cancer patients harbor SMARCA4 mutations, resulting in protein loss or loss-of-function alterations. These SMARCA4-deficient cancers are highly dependent on SMARCA2 for proliferation, growth, and survival, making SMARCA2 a promising...

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Identifiers

PMID: 40991405
DOI: 10.1158/0008-5472.CAN-25-1141

Genes

SMARCA2
SMARCA4

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