The DOI matches its Crossref record; 21 of the 21 references it cites were found in a registry or an index.
Discovery of Ledipasvir (GS-5885): A Potent, Once-Daily Oral NS5A Inhibitor for the Treatment of Hepatitis C Virus Infection
Abstract
A new class of highly potent NS5A inhibitors with an unsymmetric benzimidazole-difluorofluorene-imidazole core and distal [2.2.1]azabicyclic ring system was discovered. Optimization of antiviral potency and pharmacokinetics led to the identification of 39 (ledipasvir, GS-5885). Compound 39 (GT1a replicon EC50 = 31 pM) has an extended plasma half-life of 37-45 h in healthy volunteers and produces a rapid >3 log viral load reduction in monotherapy at oral doses of 3 mg or greater with once-daily dosing in genotype 1a HCV-infected patients. 39 has been shown to be safe and efficacious, with SVR12 rates up to 100% when used in combination with direct-acting antivirals having complementary mechanisms.
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Metadata
- Authors
- Link, J. O., Taylor, J. G., Xu, L., Mitchell, M., Guo, H., Liu, H., Kato, D., Kirschberg, T., Sun, J., Squires, N., Parrish, J., Keller, T., Yang, Z.-Y., Yang, C., Matles, M., Wang, Y., Wang, K., Cheng, G., Tian, Y., Mogalian, E., Mondou, E., Cornpropst, M., Perry, J., & Desai, M. C.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2014-01-10
- Volume
- 57
- Issue
- 5
- Pages
- 2033-2046
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2064285218
- Cited by
- 295
- References
- 21
- FWCI
- 17.98
- Type
- journal article
- Language
- en
- Open access
- closed
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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.
