APR-246 + carboplatin + pegylated liposomal doxorubicin

APR-246 + carboplatin + pegylated liposomal doxorubicin is a **combination therapy** under investigation for the treatment of cancer, especially TP53-mutant and platinum-resistant malignancies. - **APR-246** (also known as PRIMA-1MET) is a small molecule prodrug converted intracellularly to methylene quinuclidinone (MQ), which binds mutant TP53 and restores its wild-type conformation and transcriptional activity. This compound also induces various forms of programmed cell death, including apoptosis, necroptosis, and ferroptosis, and may act independently of TP53 mutation status[1][5]. - **Carboplatin** is a platinum-based DNA-alkylating agent that induces crosslinks in DNA, leading to apoptosis. - **Pegylated liposomal doxorubicin** (branded as Caelyx) is an anthracycline chemotherapeutic encapsulated within pegylated liposomes, enhancing tumor selectivity and reducing off-target toxicity. Doxorubicin itself intercalates DNA, inhibits topoisomerase 2, and generates free radicals that damage cellular macromolecules[2][4][8]. This combination regimen aims to induce cytotoxicity through complementary mechanisms: restoration of TP53 activity, direct DNA damage, and inhibition of DNA repair and replication.

Other names

carboplatinpegylated liposomal doxorubicindoxorubicin hydrochloride liposomePRIMA-1METPRIMA1METPRIMA 1MET