Drug intelligence / Profile preview

tigilanol tiglate + pembrolizumab

Development stage
Unknown
Lead developer
Qbiotics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intratumoral, Intravenous
01

Overview

Tigilanol tiglate + pembrolizumab is a combination regimen currently studied for the treatment of unresectable, advanced melanoma. Tigilanol tiglate is an intratumorally administered, plant-derived small molecule that acts primarily as a protein kinase C (PKC) activator, causing rapid tumor cell death through vascular disruption, immunogenic cell death (notably pyroptosis), and immune-mediated mechanisms. Pembrolizumab is a systemic, humanized monoclonal antibody against programmed cell death protein 1 (PD-1), functioning as an immune checkpoint inhibitor to reactivate anti-tumor immune responses. The combination is designed to enhance anti-tumor activity by combining local tumor ablation with systemic immune activation. This combination is under clinical investigation for patients with unresectable, Stage IIIB to IV M1c melanoma, including those previously treated with immune checkpoint inhibitors[1][3][5].

02

Targets

PRKCB (Protein kinase C beta)PRKCG (Protein kinase C gamma)PDCD1 (Programmed cell death protein 1 receptor)PRKCA (Protein kinase C alpha)

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