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sofosbuvir

Trade name: sovaldi

Small moleculeapprovedFast Track FDABreakthrough Therapy FDA

Approved

Dec 6, 2013

Sofosbuvir is a nucleotide analog inhibitor of hepatitis C virus NS5B polymerase - the key enzyme mediating HCV RNA replication. Sofosbuvir is a prodrug and after ingestion it is rapidly converted to GS-331007, the predominant circulating drug that accounts for greater than 90% of the systemically active drug. The compound GS-331007 is efficiently taken up by hepatocytes, whereby cellular kinases convert GS-331007 to its pharmacologically active uridine analog 5’-triphosphate form (GS-461203). This triphosphate compound mimics the natural cellular uridine nucleotide and is incorporated by the HCV RNA polymerase into the elongating RNA primer strand, resulting in chain termination. The active form GS-461203 targets the NS5B catalytic site and acts as a non-obligate chain terminator. The active compound (GS-461203) does not inhibit host DNA polymerases, RNA polymerases, or mitochondrial RNA polymerase. Sofosbuvir (alone or in in combination with other medications) is used to treat Hepatitis C. — NCATS

Clinical trial activity

332 trials · 185 clinical orgs · 2 marketing orgs

Phase 1
30
Phase 2
191
Phase 3
101
Phase 4
81

Earliest trial started Jan 1, 2010 (NCT01054729)

Timeline

2010s

  1. Jan 1, 2010

    Gilead Sciences — Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2011

    Gilead Sciences — Earliest Phase 1 Sponsor(trial)

  3. Jan 1, 2011

    Gilead Sciences — Earliest Phase 3 Sponsor(trial)

  4. Dec 6, 2013

    Gilead Sciences — Earliest FDA Approval

  5. Dec 6, 2013

    Gilead Sciences — NDA Organization

2020s

  1. Jan 27, 2022

    Teva — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

  • epclusa

    with velpatasvir

    Also known as sofosbuvir and velpatasvir

  • harvoni

    with ledipasvir

    Also known as ledipasvir and sofobuvir, ledipasvir and sofosbuvir

  • vosevi

    with velpatasvir, voxilaprevir

    Also known as sofosbuvir, velpatasvir and voxilaprevir

Approval history

  • approvedPriority reviewFast trackBreakthroughDec 6, 2013

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)OC(=O)[C@H](C)N[P@](=O)(OC[C@H]1O[C@@H](N2C=CC(=O)NC2=O)[C@](C)(F)[C@@H]1O)OC3=CC=CC=C3
Mol. weight
529.4525 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Black box warningFirst in classProdrug

Sources

Also known as

  • elbanovir
  • gs7977
  • gs7977
  • gs-7977
  • gs-7977
  • ledispavir 90 mg / sofosbuvir 400 mg
  • magicbuvir
  • psi-7977
  • psi-7977
  • psi-7977
  • s)-isopropyl 2-((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4- dihydropyrimidin-1(2h)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)- (phenoxy)phosphorylamino)propanoate
  • s)-isopropyl 2-((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4- dihydropyrimidin-1(2h)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)- (phenoxy)phosphorylamino)propanoate
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir
  • sofosbuvir / velpatasvir
  • sofosbuvir / velpatasvir
  • sofosbuvir / velpatasvir / voxilaprevi
  • sovaldi
  • sovaldi
  • sovaldi
  • sovaldi

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06953479Phase 4Jun 11, 2025Brown University, National Institute on Drug Abuse (NIDA)
NCT06533319N/AAug 1, 2024Eastern Idaho Public Health
NCT06159504Early Phase 1 (Phase 1)Mar 31, 2024Burnet Institute, Médecins du Monde, UNITAID, University of Bristol
NCT05992077N/AAug 7, 2023Government of France
NCT05248919N/AJun 1, 2023Aga Khan University, Dow University of Health Sciences, University of Bristol, University of London, University of Oxford
NCT05467826Phase 4Sep 1, 2022Peking University
NCT06306300Phase 4Jul 4, 2022Conselho Nacional de Desenvolvimento Científico e Tecnológico, Oswaldo Cruz Foundation
NCT05854511Phase 3Jun 5, 2022Ain Shams University, Cairo University
NCT05264558Phase 4May 25, 2022Cairns Hospital, University of Queensland
NCT05616598Phase 2/Phase 3 (Phase 3)Mar 1, 2022Benha University
NCT05140941Phase 4Feb 1, 2022Gilead Sciences, University of Pittsburgh
NCT05016609Phase 4Oct 31, 2021Burnet Institute
NCT04997564Phase 4Aug 31, 2021Peking University
NCT04885855Phase 2/Phase 3 (Phase 3)Mar 23, 2021Hospital Sultanah Bahiyah
NCT04535869Phase 3Dec 30, 2020Mansoura University
NCT04561063Phase 2Dec 8, 2020University of the Witwatersrand
NCT04468087Phase 2/Phase 3 (Phase 3)Dec 1, 2020Hospital do Coracao
NCT04695769Phase 4Nov 21, 2020Helwan University
NCT04773756Phase 4Nov 1, 2020Alexandria University
NCT04653818Phase 4Oct 5, 2020Alexandria University
Showing 20 of 332 trials
Page 1 / 17

Organizations

Research & Development (185)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Gilead SciencesFor profit1239652010
Bristol-Myers SquibbFor profit121232011
Janssen Pharmaceutica NVFor profit11032012
Humanity & Health Research CentreAcademic/Hospital9932015
Johnson and JohnsonFor profit9922012
Ain Shams UniversityAcademic/Hospital8732014
Harvard UniversityAcademic/Hospital8632014
People's Liberation Army of ChinaGovernment8032015
University of New South WalesAcademic/Hospital8742014
University of PittsburghAcademic/Hospital8832016
AbbVieFor profit7632014
Cairo UniversityAcademic/Hospital7232015
National Institute of Allergy and Infectious Diseases (NIAID)Government7332011
Peking UniversityAcademic/Hospital7242016
Tanta UniversityAcademic/Hospital7732016
Assiut UniversityAcademic/Hospital6642017
Genuine Research Center, EgyptFor profit6612015
Johns Hopkins UniversityAcademic/Hospital6442015
MerckFor profit6342014
University of California, San FranciscoAcademic/Hospital6422014
185 organizations
Page 1 / 10

Marketing (2)

OrganizationOrg typeRelationshipDate
Gilead SciencesFor profitNDADec 6, 2013
TevaFor profitMKTGJan 27, 2022