Therapy Detail

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Therapy Name Ravoxertinib
Synonyms
Therapy Description

Ravoxertinib (GDC-0994) is a small molecule inhibitor of ERK1 and ERK2, which may decrease tumor growth (Cancer Res October 1, 2014 74:DDT02-03, PMID: 32311798, PMID: 31848189).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Ravoxertinib GDC-0994 ERK Inhibitor (pan) 20 Ravoxertinib (GDC-0994) is a small molecule inhibitor of ERK1 and ERK2, which may decrease tumor growth (Cancer Res October 1, 2014 74:DDT02-03, PMID: 32311798, PMID: 31848189).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF V600E MAP2K1 D67N melanoma decreased response Ravoxertinib Preclinical - Cell culture Actionable In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D67N was less responsive to Ravoxertinib (GDC-0994) compared to cells expressing wild-type MAP2K1 in culture (PMID: 36442478). 36442478
BRAF V600E MAP2K1 I99_K104del melanoma decreased response Ravoxertinib Preclinical - Cell culture Actionable In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 I99_K104del was less responsive to Ravoxertinib (GDC-0994) compared to cells expressing wild-type MAP2K1 in culture (PMID: 36442478). 36442478
BRAF V600E colorectal cancer predicted - sensitive Ravoxertinib Case Reports/Case Series Actionable In a Phase I trial, two colorectal cancer patients harboring BRAF V600E achieved partial responses lasting 21 and 73 weeks following treatment with Ravoxertinib (GDC-0994) (PMID: 31848189; NCT01875705). 31848189
BRAF G469A lung adenocarcinoma resistant Ravoxertinib Preclinical - Patient cell culture Actionable In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF G469A were resistant to treatment with Ravoxertinib (GDC-0994) in culture (PMID: 32540409). 32540409
BRAF L597V lung adenocarcinoma resistant Ravoxertinib Preclinical - Patient cell culture Actionable In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF L597V were resistant to treatment with Ravoxertinib (GDC-0994) in culture (PMID: 32540409). 32540409
BRAF V600E MAP2K1 P124S melanoma decreased response Ravoxertinib Preclinical - Cell culture Actionable In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P124S was less responsive to Ravoxertinib (GDC-0994) compared to cells expressing wild-type MAP2K1 in culture (PMID: 36442478). 36442478
BRAF V600E MAP2K1 E203K melanoma decreased response Ravoxertinib Preclinical - Cell culture Actionable In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 E203K was less responsive to Ravoxertinib (GDC-0994) compared to cells expressing wild-type MAP2K1 in culture (PMID: 36442478). 36442478

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT01875705 Phase I Ravoxertinib A Dose-Escalation Study of GDC-0994 in Patients With Locally Advanced or Metastatic Solid Tumors Completed USA | FRA 0
NCT02457793 Phase I Cobimetinib Ravoxertinib A Study of the Safety, Tolerability, and Effects of Cobimetinib and GDC-0994 in Patients With Locally Advanced or Metastatic Solid Tumors Completed USA 0


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