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) 21 | 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 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 |
| BRAF V600E | melanoma | sensitive | Ravoxertinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ravoxertinib (GDC-0994) inhibited viability and colony formation in melanoma cell lines harboring BRAF V600E in culture (PMID: 38728872). | 38728872 |
| 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 | 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 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 | papillary thyroid carcinoma | sensitive | Ravoxertinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ravoxertinib (GDC-0994) inhibited viability and colony formation in papillary thyroid carcinoma cell lines harboring BRAF V600E in culture (PMID: 38728872). | 38728872 |
| 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 | anaplastic thyroid carcinoma | sensitive | Ravoxertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ravoxertinib (GDC-0994) inhibited viability and colony formation and induced cell cycle arrest in an anaplastic thyroid carcinoma cell line harboring BRAF V600E in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 38728872). | 38728872 |
| NRAS Q61K | anaplastic thyroid carcinoma | sensitive | Ravoxertinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ravoxertinib (GDC-0994) inhibited viability of an anaplastic thyroid carcinoma cell line harboring NRAS Q61K in culture (PMID: 38728872). | 38728872 |
| 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 |
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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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