Drug intelligence / Profile preview

actinium Ac 225 alpitatug satetraxetan

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Actinium Ac 225 alpitatug satetraxetan (JNJ-69086420) is a first-in-class, targeted alpha-particle radiopharmaceutical (radioimmunotherapy) developed by Johnson & Johnson in collaboration with Diaprost. It consists of alpitatug, a humanized IgG1 monoclonal antibody targeting human kallikrein-2 (hK2, encoded by the KLK2 gene), conjugated via a satetraxetan (DOTA-derivative) chelator to the alpha-emitting radioisotope actinium-225 (225Ac). hK2 is a prostate-specific serine protease highly expressed on the cell surface of prostate cancer cells with minimal expression in normal non-prostate tissues. Upon binding to hK2, the conjugate is internalized, delivering a highly cytotoxic dose of short-range alpha radiation directly to the tumor cells, causing double-strand DNA breaks and cell death. It is currently in Phase 1 clinical development for the treatment of advanced prostate cancer, including metastatic castration-resistant prostate cancer (mCRPC) and metastatic hormone-sensitive prostate cancer (mHSPC).

Other names
actinium (225Ac) alpitatug satetraxetanactinium Ac 225 alpitatug satretraxetecanactinium Ac-225 alpitatug satetraxetanactinium-225-labeled anti-kallikrein-2 h11B6actinium225-labeled anti-kallikrein-2 h11B6actinium 225-labeled anti-kallikrein-2 h11B6actinium-225-labeled h11B6actinium225-labeled h11B6actinium 225-labeled h11B6actinium-labeled anti-hK2 antibodyactinium-labeled anti-hK2 monoclonal antibodyactinium-labeled antibody targeting human kallikrein-2
02

Targets

AR (Adrenergic receptors)DNAHK2 (Hexokinase Type II)PSA (Puromycin-sensitive aminopeptidase)

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