JNJ-101684362

JNJ-101684362 (also known as HLD-0117 or JNJ-4362) is an orally administered, first-in-class regulated induced proximity targeting chimera (RIPTAC) being developed by Johnson & Johnson (following its acquisition of Halda Therapeutics) for the treatment of estrogen receptor-positive (ER+) metastatic breast cancer. Mechanistically, JNJ-101684362 is a heterobifunctional small molecule designed to simultaneously bind to the intracellular tumor-specific target protein, estrogen receptor alpha (ERα), and a pan-essential effector protein, bromodomain-containing protein 4 (BRD4). This dual binding induces the formation of a stable ternary complex, sterically hindering and inactivating BRD4 selectively within ER-expressing cancer cells, which leads to cell death while sparing healthy tissues that lack ER overexpression.

Other names

ER RIPTACestrogen receptor RIPTAC