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AT-101 is a lead conjugated targeted oncolytic peptide developed by A28 Therapeutics for the treatment of various solid tumors that overexpress Luteinizing Hormone-Releasing Hormone (LHRH) receptors. The drug is a peptide-drug conjugate consisting of a 10-amino acid LHRH targeting unit linked to an 18-amino acid positively charged lytic peptide payload known as CLYP-71. The LHRH targeting unit specifically binds to LHRH receptors on the surface of cancer cells, such as those in ovarian, prostate, breast, and endometrial cancers. Upon binding, the cationic lytic peptide is attracted to the negatively charged cancer cell membrane, leading to membrane disruption and rapid cell lysis. This mechanism is designed to selectively destroy tumor cells while sparing healthy cells. AT-101 has been evaluated in Phase 1 and Phase 2 clinical trials involving over 85 patients, demonstrating a favorable safety profile and promising clinical activity.
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