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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 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 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 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
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 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 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 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 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 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 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 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 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 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
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
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 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 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 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...
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 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 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 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 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 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 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 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 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
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 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 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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT04566393 Expanded access Ulixertinib Expanded Access to Ulixertinib (BVD-523) in Patients With Advanced MAPK Pathway-Altered Malignancies Available USA 0
NCT06411821 Phase II Ulixertinib Ulixertinib in People With Histiocytic Neoplasms Recruiting USA 0
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
NCT03417739 Phase II Ulixertinib A Phase II Study of BVD-523 in Metastatic Uveal Melanoma Active, not recruiting USA 0
NCT04488003 Phase II Ulixertinib Study of Ulixertinib for Patients With Advanced Malignancies Harboring MEK or Atypical BRAF Alterations Terminated 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
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
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
NCT05804227 Phase I Ulixertinib Window-of-Opportunity Trial of Ulixertinib for MAPK-Activated Low-Grade Gliomas in Adults Recruiting USA 0


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