Therapy Detail

Therapy Name CEP-32496
Therapy Description

RXDX-105 (CEP-32496) inhibits wild-type BRAF, BRAF V600E, c-RAF, ABL1 (and BCR-ABL), c-KIT, RET, PDGFR beta, and VEGFR2, potentially resulting in decreased tumor growth (PMID: 22319199).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
RXDX-105 AC013773|CEP-32496 ABL Inhibitor (pan) 8 ABL1 Inhibitor 4 BCR-ABL Inhibitor 23 BRAF Inhibitor 18 CRAF Inhibitor 10 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 VEGFR2 Inhibitor 34 RXDX-105 (CEP-32496) inhibits wild-type BRAF, BRAF V600E, c-RAF, ABL1 (and BCR-ABL), c-KIT, RET, PDGFR beta, and VEGFR2, potentially resulting in decreased tumor growth (PMID: 22319199).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
RET C634W thyroid medullary carcinoma sensitive CEP-32496 Preclinical - Cell culture Actionable In a preclinical study, RXDX-105 (CEP-32496) reduced phosphorylation of RET and downstream signaling and inhibited proliferation of a medullary thyroid cancer cell line harboring RET C634W in culture (PMID: 28011461). 28011461
Unknown unknown Advanced Solid Tumor not applicable CEP-32496 Phase I Actionable In a Phase I clinical trial, RXDX-105 (CEP-32496) was tolerable and demonstrated preliminary efficacy in patients with advanced solid tumors (J Clin Oncol 34, 2016 (suppl; abstr 2574)). detail...
BRAF V600E melanoma sensitive CEP-32496 Preclinical - Cell line xenograft Actionable In preclinical studies, CEP-32496 (RXDX-105) reduced tumor volume and promoted tumor regression in xenograft models of a BRAF V600E mutant human melanoma cell line (PMID: 22319199). 22319199
BRAF V600E colon carcinoma sensitive CEP-32496 Preclinical - Cell line xenograft Actionable In preclinical studies, CEP-32496 (RXDX-105) reduced tumor volume and promoted tumor regression in xenograft models of a BRAF V600E mutant human colon carcinoma cell line (PMID: 22319199). 22319199
RET rearrange Advanced Solid Tumor sensitive CEP-32496 Preclinical - Pdx Actionable In a preclinical study, CEP-32496 (RXDX-105) induced tumor regression in patient-derived xenograft models of several advanced solid tumor type with RET rearrangements (2015 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; Abstract A174). detail...
Unknown unknown non-small cell lung carcinoma not applicable CEP-32496 Phase I Actionable In a Phase I clinical trial, RXDX-105 (CEP-32496) demonstrated safety and preliminary efficacy in patients with advanced solid tumors, including 2 patients with heavily pretreated non-small cell lung cancer that achieved stable disease for greater that 6 months (AACR; Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr C188). detail...
RET rearrange non-small cell lung carcinoma sensitive CEP-32496 Clinical Study Actionable In a clinical case study, a patient with non-small cell lung cancer harboring a RET rearrangement demonstrated a sustained partial response following treatment with RXDX-105 (CEP-32496) on a Phase Ib clinical trial (PMID: 28011461). 28011461
Clinical Trial Phase Therapies Title Recruitment Status
NCT03052569 Expanded access CEP-32496 Expanded Access to RXDX-105 for Cancers With RET Alterations Temporarily not available
NCT01877811 Phase Ib/II CEP-32496 CEP-32496 in Patients With Advanced Solid Tumors in Phase 1 and Advanced Melanoma and Metastatic Colorectal Cancer in Phase 2 Active, not recruiting
NCT03784378 Phase Ib/II CEP-32496 Continued Access to RXDX-105 Recruiting