Therapy Detail
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| Therapy Name | Ulixertinib |
| Synonyms | |
| Therapy Description |
Ulixertinib (BVD-523) inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways and resulting in growth inhibition (PMID: 28939558). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Ulixertinib | BVD-523|BVD 523|BVD523 | ERK Inhibitor (pan) 21 | Ulixertinib (BVD-523) inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways and resulting in growth inhibition (PMID: 28939558). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF L597Q | lung cancer | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a partial response in a lung cancer patient harboring BRAF L597Q (PMID: 29247021; NCT01781429). | 29247021 |
| BRAF fusion | high grade glioma | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase II trial (APEC1621J), Ulixertinib (BVD-523) treatment resulted in a 6-month progression-free survival rate of 37% but no objective response in pediatric and young adult patients with advanced solid tumors harboring MAPK pathway activation, however, a patient with high grade glioma harboring a BRAF fusion achieved prolonged stable disease and remained on treatment for 15 cycles (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 3009; NCT03698994). | detail... |
| BRAF V600E | colorectal cancer | sensitive | Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited Erk signaling in colorectal cancer cells harboring BRAF V600E, resulted in cell cycle arrest in culture and tumor growth inhibition in cell line xenograft models (PMID: 28939558). | 28939558 |
| BRAF G469A | lung adenocarcinoma | resistant | Ulixertinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF G469A were resistant to treatment with Ulixertinib (BVD-523) in culture (PMID: 32540409). | 32540409 |
| BRAF mutant | melanoma | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a best response of stable disease in six melanoma patients and a partial response in three melanoma patients all harboring a BRAF mutation (PMID: 29247021; NCT01781429). | 29247021 |
| BRAF L485W | gallbladder cancer | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a complete response lasting almost 1 year in a gallbladder cancer patient harboring BRAF L485W (PMID: 29247016, PMID: 29247021; (PMID: 29247021; NCT01781429).). | 29247021 29247016 |
| BRAF V600E | central nervous system cancer | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase II trial (APEC1621J), Ulixertinib (BVD-523) treatment resulted in a 6-month progression-free survival rate of 37% but no objective response in pediatric and young adult patients with advanced solid tumors harboring MAPK pathway activation, however, a patient with glioneuronal tumor harboring a BRAF V600E achieved prolonged stable disease and remained on treatment for 9 cycles (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 3009; NCT03698994). | detail... |
| BRAF V600E MAP2K1 D67N | melanoma | decreased response | Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D67N was less responsive to Ulixertinib (BVD-523) compared to cells expressing wild-type MAP2K1 in culture (PMID: 36442478). | 36442478 |
| BRAF V600E | pancreatic ductal adenocarcinoma | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In an expanded access program (ULI-EAP-100), Ulixertinib (BVD-523) treatment resulted in clinical benefit in a patient with pancreatic ductal adenocarcinoma harboring BRAF V600E who stayed on treatment for 413 days (J Clin Oncol 40, no. 16_suppl (June 01, 2022) e15101; NCT04566393). | detail... |
| BRAF V600E MAP2K1 I99_K104del | melanoma | decreased response | Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 I99_K104del was less responsive to Ulixertinib (BVD-523) compared to cells expressing wild-type MAP2K1 in culture (PMID: 36442478). | 36442478 |
| BRAF N486_P490del | ovarian cancer | predicted - sensitive | Ulixertinib | Preclinical - Biochemical | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited metabolic activity in an ovarian cancer cell line harboring BRAF N486_P490del in culture (PMID: 37656784). | 37656784 |
| BRAF V600E | lung cancer | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a partial response in two patients with lung cancer each harboring BRAF V600E (PMID: 29247021; NCT01781429). | 29247021 |
| BRAF L485_P490delinsY | lung non-small cell carcinoma | predicted - sensitive | Ulixertinib | Preclinical - Biochemical | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited metabolic activity in a non-small cell lung cancer cell line harboring BRAF L485_P490delinsY in culture (PMID: 37656784). | 37656784 |
| BRAF V600E MAP2K1 Q56P | melanoma | sensitive | Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited proliferation of melanoma cells harboring BRAF V600E and expressing MAP2K1 Q56P in culture (PMID: 28655712). | 28655712 |
| BRAF G469A | small intestine carcinoma | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a partial response in two patients harboring BRAF G469A, including one patient with head and neck cancer and one patient with small bowel cancer (PMID: 29247021; NCT01781429). | 29247021 |
| NRAS mutant | melanoma | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a best response of stable disease in six melanoma patients and a partial response in three melanoma patients all harboring an NRAS mutation (PMID: 29247021; NCT01781429). | 29247021 |
| BRAF L597V | lung adenocarcinoma | resistant | Ulixertinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF L597V were resistant to treatment with Ulixertinib (BVD-523) in culture (PMID: 32540409). | 32540409 |
| BRAF V600E MAP2K1 E203K | melanoma | conflicting | Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited proliferation of melanoma cells harboring BRAF V600E and expressing MAP2K1 E203K in culture (PMID: 28655712). | 28655712 |
| BRAF V600E MAP2K1 E203K | melanoma | conflicting | Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 E203K was less responsive to Ulixertinib (BVD-523) compared to cells expressing wild-type MAP2K1 in culture (PMID: 36442478). | 36442478 |
| BRAF D594G | melanoma | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a clinical case study, Ulixertinib (BVD-523) treatment resulted in a histologic response allowing for surgical resection in a patient with metastatic melanoma harboring BRAF D594G (PMID: 35551160; NCT04566393). | 35551160 |
| BRAF V600E | glioblastoma | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a partial response in a patient with glioblastoma harboring BRAF V600E (PMID: 29247021; NCT01781429). | 29247021 |
| BRAF V600E | glioblastoma | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In an expanded access program (ULI-EAP-100), Ulixertinib (BVD-523) treatment resulted in clinical benefit in a patient with glioblastoma harboring BRAF V600E who stayed on treatment for 128 days (J Clin Oncol 40, no. 16_suppl (June 01, 2022) e15101; NCT04566393). | detail... |
| NRAS Q61K | neuroblastoma | predicted - sensitive | Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, neuroblastoma cell lines either harboring or expressing NRAS Q61K demonstrated moderate growth inhibition in culture when treated with Ulixertinib (BVD-523) (PMID: 32586982). | 32586982 |
| BRAF G469A | head and neck cancer | sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase I trial, treatment with Ulixertinib (BVD-523) resulted in a partial response in two patients harboring BRAF G469A, including one patient with head and neck cancer and one patient with small bowel cancer (PMID: 29247021; NCT01781429). | 29247021 |
| BRAF N486_P490del | pancreatic ductal adenocarcinoma | sensitive | Ulixertinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, a pancreatic ductal adenocarcinoma patient-derived organoid model harboring BRAF N486_P490del was sensitive to treatment with Ulixertinib (BVD-523) in culture, demonstrating decreased cell viability (PMID: 37463056). | 37463056 |
| BRAF V600E MAP2K1 V211D | melanoma | sensitive | Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited proliferation of melanoma cells harboring BRAF V600E and expressing MAP2K1 V211D in culture (PMID: 28655712). | 28655712 |
| BRAF V600E | melanoma | sensitive | Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited Erk signaling in melanoma cells harboring BRAF V600E, resulted in cell cycle arrest in culture and tumor growth inhibition in cell line xenograft models (PMID: 28939558). | 28939558 |
| BRAF V600E MAP2K1 P124S | melanoma | decreased response | Ulixertinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P124S was less responsive to Ulixertinib (BVD-523) compared to cells expressing wild-type MAP2K1 in culture (PMID: 36442478). | 36442478 |
| BRAF V487_P492delinsA | pancreatic carcinoma | predicted - sensitive | Ulixertinib | Preclinical - Biochemical | Actionable | In a preclinical study, Ulixertinib (BVD-523) inhibited metabolic activity in a pancreatic carcinoma cell line harboring BRAF V487_P492delinsA in culture (PMID: 37656784). | 37656784 |
| BRAF fusion | low grade glioma | predicted - sensitive | Ulixertinib | Case Reports/Case Series | Actionable | In a Phase II trial (APEC1621J), Ulixertinib (BVD-523) treatment resulted in a 6-month progression-free survival rate of 37% but no objective response in pediatric and young adult patients with advanced solid tumors harboring MAPK pathway activation, however, a patient with low grade glioma harboring a BRAF fusion achieved prolonged stable disease and remained on treatment for 7 cycles (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 3009; NCT03698994). | detail... |
| BRAF V600E | pleomorphic xanthoastrocytoma | sensitive | Ulixertinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Ulixertinib (BVD-523) reduced metabolic activity and inhibited MAPK pathway activity in a pleomorphic xanthoastrocytoma cell line harboring BRAF V600E in culture, and inhibited tumor growth and improved survival compared to vehicle (48.5 days vs 30 days, respectively) in a xenograft model (PMID: 35882450). | 35882450 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02296242 | Phase Ib/II | Ulixertinib | Phase 1/2 Study of the ERK1/2 Inhibitor BVD-523 in Patients With Acute Myelogenous Leukemia or Myelodysplastic Syndromes | Completed | USA | 0 |
| NCT04566393 | Expanded access | Ulixertinib | Expanded Access to Ulixertinib (BVD-523) in Patients With Advanced MAPK Pathway-Altered Malignancies | Available | USA | 0 |
| NCT03155620 | Phase II | Tazemetostat Larotrectinib LY3023414 Vemurafenib Palbociclib Olaparib Ulixertinib Erdafitinib Selumetinib Ensartinib | Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial) | Recruiting | USA | CAN | AUS | 1 |
| NCT03698994 | Phase II | Ulixertinib | Ulixertinib in Treating Patients With Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With MAPK Pathway Mutations (A Pediatric MATCH Treatment Trial) | Active, not recruiting | USA | 1 |
| NCT04488003 | Phase II | Ulixertinib | Study of Ulixertinib for Patients With Advanced Malignancies Harboring MEK or Atypical BRAF Alterations | Terminated | USA | 0 |
| NCT03417739 | Phase II | Ulixertinib | A Phase II Study of BVD-523 in Metastatic Uveal Melanoma | Active, not recruiting | USA | 0 |
| NCT05804227 | Phase I | Ulixertinib | Window-of-Opportunity Trial of Ulixertinib for MAPK-Activated Low-Grade Gliomas in Adults | Recruiting | USA | 0 |
| NCT01781429 | Phase Ib/II | Ulixertinib | Phase I Dose-Escalation, Safety, Pharmacokinetic and Pharmacodynamic Study of BVD-523 in Patients With Advanced Malignancies | Completed | USA | 0 |
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