The current standard of care for HIV is a combination of drugs, known as highly active antiretroviral therapy (HAART). A frequent component of HAART is a non-nucleoside reverse transcriptase inhibitor (NNRTI) which prevent conversion of viral RNA into DNA. This presentation will discuss the discovery, early and late-development of doravirine, a new NNRTI for the treatment of HIV approved by the FDA in 2018 for two products, Delstrigo and Pifeltro. A complete picture of key chemistry over the lifetime of the project will be highlighted. Key structure activity relationships, as well as critical optimized pharmacokinetic and physico-chemical parameters will be presented. The evolution of the synthesis methodologies used throughout the lifetime of the program will also be elaborated, including the early development supply route and our efforts toward the establishment of the manufacturing process.

The discovery and development of doravirine

ACS Fall 2021

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