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Therapy Name RXDX-105
Synonyms
Therapy Description

Agerafenib (RXDX-105) 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, PMID: 31695841).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
RXDX-105 AC013773|CEP-32496|Agerafenib ABL Inhibitor (pan) 9 ABL1 Inhibitor 8 BCR-ABL Inhibitor 32 BRAF Inhibitor 25 CRAF Inhibitor 12 KIT Inhibitor 57 PDGFR-beta Inhibitor 14 RET Inhibitor 53 VEGFR2 Inhibitor 37 Agerafenib (RXDX-105) 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, PMID: 31695841).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
RET rearrange Advanced Solid Tumor sensitive RXDX-105 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...
RET rearrange lung non-small cell carcinoma predicted - sensitive RXDX-105 Case Reports/Case Series 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; NCT01877811). 28011461
RET rearrange lung non-small cell carcinoma predicted - sensitive RXDX-105 Phase I Actionable In a Phase Ib trial, treatment with RXDX-105 (CEP-32496) resulted in an overall response rate of 19% (6/31) and stable disease in 39% (12/31) of patients with treatment-naive non-small cell lung cancer harboring a RET fusion (PMID: 30487236; NCT01877811) 30487236
EML4 - RET lung adenocarcinoma sensitive RXDX-105 Preclinical - Patient cell culture Actionable In a preclinical study, a patient-derived lung adenocarcinoma cell line harboring EML4-RET was sensitive to treatment with Agerafenib (RXDX-105) in culture, demonstrating decreased Akt phosphorylation and induction of apoptosis (PMID: 33795352). 33795352
BRAF V600E colon carcinoma sensitive RXDX-105 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 C634W medullary thyroid carcinoma sensitive RXDX-105 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
BRAF V600E melanoma sensitive RXDX-105 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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT03784378 Phase I RXDX-105 Continued Access to RXDX-105 Completed USA 0
NCT03052569 Expanded access RXDX-105 Expanded Access to RXDX-105 for Cancers With RET Alterations No longer available USA 0
NCT01877811 Phase Ib/II RXDX-105 CEP-32496 in Patients With Advanced Solid Tumors in Phase 1 and Advanced Melanoma and Metastatic Colorectal Cancer in Phase 2 Completed USA 0


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