Sofituzumab vedotin (DMUC5754A) is a MMAE-containing anti-MUC16 antibody-drug conjugate (ADC) with a protease-cleavable linker. Sofituzumab vedotin can be used for the research of cancer.
Sofituzumab vedotin (DMUC5754A) is an antibody–drug conjugate (ADC) that contains the humanized IgG1 anti-MUC16 monoclonal antibody and a potent anti-mitotic agent, monometl auristatin E (MMAE), linked through a protease-labile linker, maleimidocaproyl-valine-citrulline-p-aminobenzyloxycarbonyl[2].Sofituzumab vedotin (3A5-VC-MMAE; 0.1-10000ng/mL; 3 or 5 days) inhibits OVCAR-3 and PC3/MUC16TMlong cells proliferation in a dose-dependent manner[3].
Sofituzumab vedotin (3A5-VC-MMAE; 2 and 2.8 mg/kg; IV; once weekly for 3 or 4 total doses) shows potent anti-tumor activity in MUC16-expressing human OVCAR-3 mouse xenograft models[3].
References:
[1]. Manzano A, et al. Antibody-Drug Conjugates: A Promising Novel Therapy for the Treatment of Ovarian Cancer. Cancers (Basel). 2020 Aug 9;12(8):2223.
[2]. Liu JF, et al. Phase I study of safety and pharmacokinetics of the anti-MUC16 antibody-drug conjugate DMUC5754A in patients with platinum-resistant ovarian cancer or unresectable pancreatic cancer. Ann Oncol. 2016 Nov;27(11):2124-2130.
[3]. Chen Y, et al. Armed antibodies targeting the mucin repeats of the ovarian cancer antigen, MUC16, are highly efficacious in animal tumor models. Cancer Res. 2007 May 15;67(10):4924-32.