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|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|RXDX-105||AC013773|CEP-32496|Agerafenib||ABL Inhibitor (pan) 8 ABL1 Inhibitor 6 BCR-ABL Inhibitor 27 BRAF Inhibitor 20 CRAF Inhibitor 12 KIT Inhibitor 51 PDGFR-beta Inhibitor 13 RET Inhibitor 39 VEGFR2 Inhibitor 35||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).|
|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...|
|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|
|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|
|Unknown unknown||lung non-small cell carcinoma||not applicable||RXDX-105||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||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|
|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|
|Unknown unknown||Advanced Solid Tumor||not applicable||RXDX-105||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...|
|RET C634W||thyroid gland medullary 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|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status||Covered Countries||Other Countries|
|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|
|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|