Applying an intensive structure-activity relationship (SAR) study, a promising IDPP .. In order to develop novel antiviral drugs against HBV, new compounds will. Figure 1 shows the chemical structure of sofosbuvir. ST amino acid change decreases the inhibitory activity of sofosbuvir. .. Gilead Sciences (the developer of both drugs) submitted the . Disclosure: The authors report that they have no commercial or financial relationships in regard to this article. Request PDF on ResearchGate | Structure-Activity Relationship (SAR) Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug.
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Sofosbuvir - Wikipedia
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Therefore, inducers of intestinal P-glycoprotein, such as rifampicin and St. John's wortcould reduce the absorption of sofosbuvir. Thus, coadministration is not recommended.SAR of acetylcholine / structural activity relationship of acetylcholine/ SAR of parasympathomimetic
Pharmacokinetics[ edit ] Sofosbuvir is only administered orally. The peak concentration after oral administration is 0. The half life of sofosbuvir is 0. This low potency arises in part because the enzymatic addition of the first of the three phosphate groups of the triphosphate is slow.
The design of sofosbuvir, based on the ProTide approach, avoids this slow step by building the first phosphate group into the structure of the drug during synthesis.
Additional groups are attached to the phosphorus to temporarily mask the two negative charges of the phosphate group, thereby facilitating entry of the drug into the infected cell. As sofosbuvir clinical development progressed, physicians began to "warehouse" people in anticipation of its availability. They specifically asked Gilead CEO John Martin to "explain how the drug was priced, what discounts are being made available to low-income patients and government health programs, and the potential impact to public health by insurers blocking or delaying access to the medicine because of its cost.