Presatovir: A Novel Fusion Inhibitor for Respiratory Syncytial Virus

Presatovir: A Novel Fusion Inhibitor for Respiratory Syncytial Virus

Presatovir, also known by its developmental code GS-5806, is an investigational antiviral medication designed to combat Respiratory Syncytial Virus (RSV). RSV is a common respiratory pathogen that can cause severe lung infections, particularly in infants and elderly populations. Presatovir represents a targeted approach to stopping the virus before it can infect healthy cells.

Mechanism of Action

Presatovir functions as a fusion inhibitor. In the viral life cycle, fusion is the critical process where the viral envelope merges with the host cell membrane, allowing the viral genetic material to enter the cell. By blocking this specific step, Presatovir prevents the virus from gaining entry into the host's cells, thereby halting the replication process and reducing the overall viral load in the body.

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Clinical Development and Status

The drug has undergone rigorous testing to evaluate its safety and efficacy. To date, Presatovir has shown promising results in Phase II clinical trials, which are designed to assess the drug's effectiveness in a larger group of patients and further evaluate its safety profile. In the United States, its legal status is currently classified as an Investigational New Drug (IND), meaning it is still undergoing the necessary regulatory reviews and trials before it can be approved for general public use.

Chemical and Physical Properties

Presatovir is a complex organic molecule with a specific chemical structure designed for high affinity to its viral target. Its molecular architecture includes a pyrazolo[1,5-a]pyrimidine core and a methanesulfonamide group, which contribute to its biological activity.

Chemical Profile of Presatovir (GS-5806)
Property Detail
IUPAC Name N-[2-[(2S)-2-[5-[(3S)-3-aminopyrrolidin-1-yl]-6-methylpyrazolo[1,5-a]pyrimidin-2-yl]piperidine-1-carbonyl]-4-chlorophenyl]methanesulfonamide
Molecular Formula C24H30ClN7O3S
Molar Mass 532.06 g·mol
CAS Number 1353625-73-6
PubChem CID 58029842
UNII 9628AJ27JA

Key Facts

  • Primary Target: Respiratory Syncytial Virus (RSV).
  • Drug Class: Fusion inhibitor.
  • Development Code: GS-5806.
  • Clinical Stage: Promising results observed in Phase II trials.
  • Regulatory Status: Investigational New Drug (US).
  • Molecular Weight: 532.06 g/mol.

Frequently Asked Questions

What is Presatovir?

Presatovir (GS-5806) is an antiviral drug currently being investigated as a treatment for infections caused by the Respiratory Syncytial Virus (RSV).

How does Presatovir work?

It acts as a fusion inhibitor, which means it prevents the RSV virus from fusing its membrane with the host cell membrane, effectively blocking the virus from entering the cell.

Is Presatovir available for prescription?

No, it is currently listed as an Investigational New Drug in the United States and is not yet approved for general clinical use.

What stage of testing has Presatovir completed?

Presatovir has shown promising results in Phase II clinical trials, which focus on efficacy and safety in a targeted patient group.

What is the chemical formula of Presatovir?

The chemical formula for Presatovir is C24H30ClN7O3S.

References

  1. Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, et al. (February 2015). "Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study". Journal of Medicinal Chemistry. 58 (4): 1630–1643. doi:10.1021/jm5017768. PMID 25574686.
  2. Yamaguchi-Sasaki T, Tamura Y, Ogata Y, Kawaguchi T, Kurosaka J, Sugaya Y, et al. (2020). "Design and Synthesis of 2-(1-Alkylaminoalkyl)pyrazolo[1,5-a]pyrimidines as New Respiratory Syncytial Virus Fusion Protein Inhibitors". Chemical & Pharmaceutical Bulletin. 68 (4): 345–362. doi:10.1248/cpb.c19-00895. PMID 32238652. S2CID 214769862.
  3. Marty FM, Chemaly RF, Mullane KM, Lee DG, Hirsch HH, Small CB, et al. (December 2019). "A Phase 2b, Randomized, Double-blind, Placebo-Controlled Multicenter Study Evaluating Antiviral Effects, Pharmacokinetics, Safety, and Tolerability of Presatovir in Hematopoietic Cell Transplant Recipients with Respiratory Syncytial Virus (RSV) Infection of the Lower Respiratory Tract". Clinical Infectious Diseases. doi:10.1093/cid/ciz1167. PMC 7108198. PMID 31915807.
  4. Stray K, Perron M, Porter DP, Anderson F, Lewis SA, Perry J, et al. (January 2020). "Drug resistance assessment following administration of RSV fusion inhibitor presatovir to participants experimentally infected with respiratory syncytial virus". The Journal of Infectious Diseases. doi:10.1093/infdis/jiaa028. PMID 31971597.