Drug intelligence / Profile preview

RP-6306 + RP-3500

Development stage
Unknown
Lead developer
Repare Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

**RP-6306 + RP-3500** is an investigational, oral combination therapy targeting advanced solid tumors, particularly those with *CCNE1* amplification such as ovarian and endometrial cancers[1][3][7]. RP-6306 (lunresertib) is a **PKMYT1 inhibitor**, interfering with the cell cycle by inhibiting PKMYT1, which regulates CDK1 activity via phosphorylation[5][8]. RP-3500 (camonsertib) is an **ATR inhibitor**, blocking ATR kinase involved in DNA damage response and cell cycle checkpoint activation[1][7]. The combination synergizes to increase CDK1 activation, induce premature mitosis, DNA damage, and apoptosis specifically in cancer cells with *CCNE1* amplification, exploiting synthetic lethal interactions[1][2]. Developed primarily for patients with advanced solid tumors—including ovarian and endometrial cancers—who have limited options due to therapy resistance[1][3].

Brand names
lunresertibcamonsertib
Other names
RP-6306 + RP-3500lunresertib + camonsertib
02

Targets

PKMYT1 (Protein kinase membrane associated tyrosine/threonine 1)

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