The DOI matches its Crossref record; 43 of the 43 references it cites were found in a registry or an index.
First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study
Abstract
Ulixertinib (BVD-523) is an ERK1/2 kinase inhibitor with potent preclinical activity in BRAF- and RAS-mutant cell lines. In this multicenter phase I trial (NCT01781429), 135 patients were enrolled to an accelerated 3 + 3 dose-escalation cohort and six distinct dose-expansion cohorts. Dose escalation included 27 patients, dosed from 10 to 900 mg twice daily and established the recommended phase II dose (RP2D) of 600 mg twice daily. Ulixertinib exposure was dose proportional to the RP2D, which provided near-complete inhibition of ERK activity in whole blood. In the 108-patient expansion cohort, 32% of patients required dose reduction. The most common treatment-related adverse events were diarrhea (48%), fatigue (42%), nausea (41%), and dermatitis acneiform (31%). Partial responses were seen in 3 of 18 (17%) patients dosed at or above maximum tolerated dose and in 11 of 81 (14%) evaluable patients in dose expansion. Responses occurred in patients with NRAS-, BRAF V600–, and non–V600 BRAF-mutant solid tumors. Significance: Here, we describe the first-in-human dose-escalation study of an ERK1/2 inhibitor for the treatment of patients with advanced solid tumors. Ulixertinib has an acceptable safety profile with favorable pharmacokinetics and has shown early evidence of clinical activity in NRAS- and BRAF V600- and non-V600–mutant solid-tumor malignancies. Cancer Discov; 8(2); 184–95. ©2017 AACR. See related commentary by Smalley and Smalley, p. 140. This article is highlighted in the In This Issue feature, p. 127
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Mutations of the BRAF gene in human cancer
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Combination of ERK and autophagy inhibition as a treatment approach for pancreatic cancer
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Metadata
- Authors
- Sullivan, R. J., Infante, J. R., Janku, F., Wong, D. J. L., Sosman, J. A., Keedy, V., Patel, M. R., Shapiro, G. I., Mier, J. W., Tolcher, A. W., Wang-Gillam, A., Sznol, M., Flaherty, K., Buchbinder, E., Carvajal, R. D., Varghese, A. M., Lacouture, M. E., Ribas, A., Patel, S. P., DeCrescenzo, G. A., Emery, C. M., Groover, A. L., Saha, S., Varterasian, M., Welsch, D. J., Hyman, D. M., & Li, B. T.
- Venue
- Cancer Discovery
- Published
- 2018-02-01
- Volume
- 8
- Issue
- 2
- Pages
- 184-195
- ISSN
- 2159-8274 (ISSN-L)
- 2159-8290
- OpenAlex
- W2774483419
- Cited by
- 426
- References
- 43
- FWCI
- 13.59
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study. https://app.cochat.ai/papers/10.1158/2159-8290.cd-17-1119
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- Sullivan, R. J., Infante, J. R., Janku, F., Wong, D. J. L., Sosman, J. A., Keedy, V., Patel, M. R., Shapiro, G. I., Mier, J. W., Tolcher, A. W., Wang-Gillam, A., Sznol, M., Flaherty, K., Buchbinder, E., Carvajal, R. D., Varghese, A. M., Lacouture, M. E., Ribas, A., Patel, S. P., . . . Li, B. T. (2018). First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study. Cancer Discovery. https://doi.org/10.1158/2159-8290.cd-17-1119
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
