Drug intelligence / Profile preview

guadecitabine + pembrolizumab

Development stage: Unknown
Lead developer: Astex Pharmaceuticals
Modality: Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration: Subcutaneous, Intravenous

Overview

A combination therapy consisting of guadecitabine, a second-generation DNA hypomethylating agent, and pembrolizumab, an immune checkpoint inhibitor. This combination has shown promise in reversing resistance to immunotherapy in various solid tumors, particularly non-small cell lung cancer. The recommended Phase 2 dose is guadecitabine 30 mg/m² (days 1-4) with pembrolizumab 200 mg on day 1 every 3 weeks.

Targets

DNMT3A (DNA methyltransferase 3 alpha)DNMT1 (DNA (cytosine-5)-methyltransferase 1)PDCD1 (Programmed cell death protein 1 receptor)DNMT3B (DNA (cytosine-5)-methyltransferase 3B)

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