DNA polymerase theta inhibitor RP-3467

An orally bioavailable inhibitor of DNA polymerase (pol) theta, with potential chemosensitizing and antineoplastic activities. Upon oral administration, pol theta inhibitor RP-3467 specifically targets, binds to and inhibits the activity of pol theta. This prevents pol theta-mediated repair of double-stranded DNA breaks via the microhomology-mediated end joining (MMEJ) process. This causes apoptosis and inhibits proliferation in cancer cells. RP-3467 may have a synergistic effect if administered in combination with agents that cause DNA damage. Pol theta plays a key role in DNA synthesis and repair that is highly expressed in cancer cells while nearly absent in most healthy tissues. It plays a key role in cancer cell survival.