The DOI matches its Crossref record; 39 of the 39 references it cites were found in a registry or an index.
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
Open accessAbstract
Aberrant activation of Bruton’s tyrosine kinase (BTK) plays an important role in pathogenesis of B-cell lymphomas, suggesting that inhibition of BTK is useful in the treatment of hematological malignancies. The discovery of a more selective on-target covalent BTK inhibitor is of high value. Herein, we disclose the discovery and preclinical characterization of a potent, selective, and irreversible BTK inhibitor as our clinical candidate by using in vitro potency, selectivity, pharmacokinetics (PK), and in vivo pharmacodynamic for prioritizing compounds. Compound BGB-3111 ( 31a, Zanubrutinib) demonstrates (i) potent activity against BTK and excellent selectivity over other TEC, EGFR and Src family kinases, (ii) desirable ADME, excellent in vivo pharmacodynamic in mice and efficacy in OCI-LY10 xenograft models.
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Metadata
- Authors
- Guo, Y., Liu, Y., Hu, N., Yu, D., Zhou, C., Shi, G., Zhang, B., Wei, M., Liu, J., Luo, L., Tang, Z., Song, H., Guo, Y., Liu, X., Su, D., Zhang, S., Song, X., Zhou, X., Hong, Y., Chen, S., Cheng, Z., Young, S., Wei, Q., Wang, H., Wang, Q., Lv, L., Wang, F., Xu, H., Sun, H., Xing, H., Li, N., Zhang, W., Wang, Z., Liu, G., Sun, Z., Zhou, D., Li, W., Liu, L., Wang, L., & Wang, Z.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2019-08-05
- Volume
- 62
- Issue
- 17
- Pages
- 7923-7940
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2972482801
- Cited by
- 359
- References
- 39
- FWCI
- 18.18
- Type
- journal article
- Language
- en
- Open access
- green
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- Guo, Y., Liu, Y., Hu, N., Yu, D., Zhou, C., Shi, G., Zhang, B., Wei, M., Liu, J., Luo, L., Tang, Z., Song, H., Guo, Y., Liu, X., Su, D., Zhang, S., Song, X., Zhou, X., Hong, Y., . . . Wang, Z. (2019). Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.9b00687
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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.
