Drug intelligence / Profile preview

abemaciclib + lutetium Lu 177 vipivotide tetraxetan

Development stage: Unknown
Lead developer: Novartis
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration: Oral, Intravenous

Overview

Abemaciclib + lutetium Lu 177 vipivotide tetraxetan is a combination therapy being investigated for the treatment of metastatic castration-resistant prostate cancer (mCRPC). This regimen utilizes abemaciclib, a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), as a priming agent to upregulate the expression of prostate-specific membrane antigen (PSMA) on tumor cells. Following this upregulation, lutetium Lu 177 vipivotide tetraxetan (Pluvicto), a PSMA-targeted radioligand therapy, is administered. The radioligand binds to the PSMA receptors and delivers targeted beta-particle radiation (from the lutetium-177 isotope), leading to DNA damage and apoptosis in the cancer cells. This combination approach aims to enhance the therapeutic efficacy of radioligand therapy by increasing the density of the target antigen on the cell surface. The treatment is currently being evaluated in clinical trials sponsored by investigators such as Vadim S. Koshkin.

Brand names: VerzenioPluvicto
Other names: Abemaciclib + 177Lu-PSMA-617Abemaciclib + Lutetium Lu 177-PSMA-617Abemaciclib + lutetium (177Lu) vipivotide tetraxetan

Targets

PSMA (Prostate-specific membrane antigen)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)

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