Drug intelligence / Profile preview

vemurafenib + KTN3379

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

Overview

Vemurafenib + KTN3379 is an investigational combination therapy comprising vemurafenib, a small molecule BRAF kinase inhibitor, and KTN3379 (also known as CDX-3379), a human monoclonal antibody targeting HER3 (ErbB3). The combination is designed to provide dual pathway inhibition in cancers driven by BRAF mutations, specifically addressing resistance mechanisms mediated by HER3 upregulation, which may limit the efficacy of BRAF inhibition alone. Preclinical and pilot clinical studies focused on BRAF^V600E^ mutated, radioiodine-refractory thyroid carcinoma, with the aim of restoring radioactive iodine (RAI) uptake in these patients. Vemurafenib inhibits BRAF activity in the MAPK signaling pathway, while KTN3379 blocks HER3, potentially enhancing redifferentiation and RAI incorporation for targeted radiotherapy[1][4][7]. The combination has not received regulatory approval and has been evaluated in early-phase clinical trials.

Brand names
Zelboraf
Other names
vemurafenib + CDX-3379
02

Targets

ERBB3 (Erb-b2 receptor tyrosine kinase 3)BRAF V600E

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