Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 12, Issue 1, Pages 101-110Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op7002198
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TRI-999 is a HIV fusion inhibitory peptide designed to improve upon the efficacy and convenience of Enfuvirtide (ENF, Fuzeon), the first approved HIV entry inhibitor. Derived from a gp41 HR2 region partially overlapping, the ENF sequence, TRI-999 is modified using a fatty acid conjugation strategy through a poly(ethylene glycol) (PEG) linker to maintain potency while achieving the desired PK. Synthetic route comparison, process development, and GMP manufacturing at the kilo scale of TRI-999 are reported.
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