ledipasvir Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals, hepatitis C Virus (HCV) NS5A inhibitors 4899 1256388-51-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ledipasvir
  • GS-5885
an inhibitor of the HCV NS5A protein, which is required for viral replication
  • Molecular weight: 889.02
  • Formula: C49H54F2N8O6
  • CLOGP: 6.71
  • LIPINSKI: 3
  • HAC: 14
  • HDO: 4
  • TPSA: 174.64
  • ALOGS: -5.36
  • ROTB: 12

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Hosey CM, Chan R, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Dec. 4, 2014 EMA
Oct. 10, 2014 FDA GILEAD SCIENCES INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Headache 2013.61 21.17 1408 12806 535413 52799439
Fatigue 1538.65 21.17 1365 12849 729141 52605711
Hepatocellular carcinoma 749.23 21.17 172 14042 2908 53331944
Hepatitis C 630.87 21.17 174 14040 6327 53328525
Insomnia 242.88 21.17 273 13941 186799 53148053
Genotype drug resistance test positive 204.59 21.17 44 14170 540 53334312
Nausea 171.46 21.17 513 13701 755578 52579274
Hepatic encephalopathy 134.11 21.17 63 14151 10796 53324056
Product dose omission issue 124.93 21.17 200 14014 191420 53143432
Hepatitis C virus test positive 124.58 21.17 24 14190 161 53334691
Ascites 111.29 21.17 89 14125 39646 53295206
Oesophageal varices haemorrhage 105.31 21.17 30 14184 1223 53333629
Diarrhoea 81.36 21.17 355 13859 625191 52709661
Hepatic cancer recurrent 81.35 21.17 14 14200 44 53334808
Dyspepsia 76.94 21.17 99 14115 77501 53257351
Hepatitis B reactivation 67.84 21.17 24 14190 1984 53332868
Rheumatoid arthritis 64.93 21.17 5 14209 314526 53020326
Hepatic cirrhosis 56.12 21.17 43 14171 17979 53316873
Hepatic cancer 51.67 21.17 23 14191 3478 53331374
Drug hypersensitivity 50.02 21.17 6 14208 265236 53069616
Product use complaint 44.48 21.17 18 14196 2152 53332700
Glomerular filtration rate decreased 40.93 21.17 31 14183 12736 53322116
Treatment failure 36.37 21.17 95 14119 128308 53206544
Liver transplant 35.57 21.17 16 14198 2478 53332374
Toxicity to various agents 34.68 21.17 8 14206 219590 53115262
Hepatic failure 34.39 21.17 45 14169 35761 53299091
Portal vein thrombosis 31.72 21.17 15 14199 2604 53332248
Neutropenia 31.52 21.17 3 14211 159182 53175670
Off label use 30.82 21.17 49 14165 472163 52862689
Irritability 28.33 21.17 38 14176 30915 53303937
Pruritus 25.36 21.17 149 14065 293683 53041169
Renal impairment 24.97 21.17 63 14151 83255 53251597
Cryoglobulinaemia 24.28 21.17 8 14206 533 53334319
Varices oesophageal 24.01 21.17 13 14201 2999 53331853
Swelling 23.12 21.17 11 14203 191094 53143758
Hypersensitivity 22.75 21.17 14 14200 210651 53124201
Arthropathy 22.63 21.17 5 14209 141448 53193404
Infection 22.27 21.17 9 14205 172196 53162656
Abnormal dreams 21.98 21.17 20 14194 10581 53324271
Complications of transplanted lung 21.27 21.17 6 14208 236 53334616

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Headache 3088.06 18.62 1728 17926 194469 32299403
Fatigue 3034.35 18.62 2105 17549 348596 32145276
Hepatitis C 1960.39 18.62 592 19062 12926 32480946
Hepatocellular carcinoma 1143.82 18.62 368 19286 9902 32483970
Treatment failure 492.57 18.62 302 19352 38861 32455011
Genotype drug resistance test positive 381.86 18.62 106 19548 1675 32492197
Drug ineffective 358.65 18.62 741 18913 382736 32111136
Insomnia 308.71 18.62 340 19314 100008 32393864
Hepatitis C virus test positive 211.36 18.62 50 19604 397 32493475
Nausea 195.59 18.62 526 19128 320323 32173549
Hepatic cirrhosis 172.05 18.62 114 19540 16695 32477177
Product dose omission issue 165.70 18.62 253 19401 102322 32391550
Ascites 140.50 18.62 146 19508 40045 32453827
Viral mutation identified 124.07 18.62 52 19602 2967 32490905
Liver transplant 123.74 18.62 51 19603 2789 32491083
Hepatitis B reactivation 98.46 18.62 46 19608 3403 32490469
Hypotension 90.35 18.62 12 19642 216098 32277774
Oesophageal varices haemorrhage 89.51 18.62 42 19612 3137 32490735
Dyspepsia 84.43 18.62 102 19552 32953 32460919
Hepatic cancer recurrent 82.66 18.62 23 19631 366 32493506
Toxicity to various agents 69.53 18.62 12 19642 178029 32315843
Hepatic encephalopathy 62.87 18.62 60 19594 14835 32479037
Pneumonia 61.35 18.62 75 19579 355177 32138695
Febrile neutropenia 59.85 18.62 3 19651 119563 32374309
Hepatic cancer 59.67 18.62 43 19611 7197 32486675
Off label use 59.10 18.62 59 19595 306261 32187611
Abdominal discomfort 52.33 18.62 105 19549 52519 32441353
Irritability 51.72 18.62 69 19585 24585 32469287
Focal segmental glomerulosclerosis 51.48 18.62 25 19629 2015 32491857
General physical health deterioration 44.46 18.62 8 19646 115251 32378621
Diarrhoea 44.17 18.62 373 19281 364429 32129443
Glomerular filtration rate decreased 43.74 18.62 46 19608 12765 32481107
Intentional dose omission 43.19 18.62 23 19631 2251 32491621
Hepatic failure 41.37 18.62 76 19578 35604 32458268
White blood cell count decreased 40.70 18.62 4 19650 91194 32402678
Dyspnoea 37.81 18.62 104 19550 361941 32131931
Hepatitis C RNA positive 36.99 18.62 11 19643 224 32493648
Malignant neoplasm progression 33.60 18.62 4 19650 78492 32415380
Pyrexia 32.58 18.62 93 19561 319875 32173997
Influenza like illness 30.44 18.62 57 19597 27083 32466789
Complications of transplanted lung 30.05 18.62 9 19645 188 32493684
Ectopic kidney 29.76 18.62 7 19647 54 32493818
Chronic hepatitis C 28.59 18.62 11 19643 501 32493371
Alpha 1 foetoprotein increased 28.02 18.62 12 19642 722 32493150
Drug abuse 28.00 18.62 7 19647 80236 32413636
Therapy cessation 27.89 18.62 41 19613 15972 32477900
Neutropenia 27.77 18.62 27 19627 142148 32351724
Disease progression 27.68 18.62 9 19645 86853 32407019
Fall 27.31 18.62 48 19606 196153 32297719
Myalgia 27.12 18.62 109 19545 81121 32412751
Laryngomalacia 25.27 18.62 9 19645 329 32493543
Dry mouth 25.01 18.62 49 19605 24070 32469802
Drug hypersensitivity 24.48 18.62 7 19647 73393 32420479
Constipation 24.44 18.62 145 19509 126228 32367644
Hepatic fibrosis 24.27 18.62 19 19635 3599 32490273
Cryoglobulinaemia 23.84 18.62 9 19645 389 32493483
Migraine 23.20 18.62 35 19619 13950 32479922
Abnormal dreams 22.78 18.62 27 19627 8537 32485335
Tachycardia 22.20 18.62 10 19644 79078 32414794
Cardiac failure 22.20 18.62 14 19640 91659 32402213
Plasma cell myeloma 22.20 18.62 4 19650 57610 32436262
Pancytopenia 22.00 18.62 14 19640 91221 32402651
Hypoxia 21.48 18.62 3 19651 52129 32441743
Respiratory failure 21.33 18.62 20 19634 107162 32386710
Erythema 21.09 18.62 12 19642 83093 32410779
Extra dose administered 20.97 18.62 17 19637 3386 32490486
Ammonia increased 20.79 18.62 19 19635 4445 32489427
Tinnitus 20.31 18.62 37 19617 17212 32476660
Drug interaction 19.73 18.62 210 19444 217975 32275897
Deep vein thrombosis 19.60 18.62 7 19647 63706 32430166
Virologic failure 19.38 18.62 17 19637 3770 32490102
Oxygen saturation decreased 19.28 18.62 3 19651 48096 32445776
Product use complaint 19.02 18.62 11 19643 1263 32492609
Product use in unapproved indication 18.90 18.62 15 19639 87189 32406683
Platelet count decreased 18.84 18.62 25 19629 114566 32379306
Blood pressure decreased 18.72 18.62 4 19650 51076 32442796
Completed suicide 18.72 18.62 17 19637 92500 32401372
Pulmonary embolism 18.62 18.62 14 19640 83645 32410227

Pharmacologic Action:

SourceCodeDescription
ATC J05AP51 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA EPC N0000191256 Hepatitis C Virus NS5A Inhibitor
CHEBI has role CHEBI:36044 anti-virus drug
CHEBI has role CHEBI:64924 hepatitis C protease inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic hepatitis C indication 128302006

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.48 acidic
pKa2 13.1 acidic
pKa3 13.41 acidic
pKa4 13.92 acidic
pKa5 6.07 Basic
pKa6 5.39 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8334270 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8580765 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8735372 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 9085573 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8334270 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8580765 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8735372 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 9085573 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8334270 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8580765 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8735372 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 9085573 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8334270 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8580765 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8735372 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 9085573 March 21, 2028 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 7964580 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8633309 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8889159 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 7964580 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8633309 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8889159 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 7964580 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8633309 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8889159 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 7964580 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8633309 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8889159 March 26, 2029 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8273341 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8822430 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8841278 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 9511056 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8273341 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8822430 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8841278 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 9511056 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8273341 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8822430 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8841278 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 9511056 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8273341 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8822430 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8841278 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 9511056 May 12, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 9284342 Sept. 13, 2030 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 9284342 Sept. 13, 2030 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 9284342 Sept. 13, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 9284342 Sept. 13, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 8618076 Dec. 11, 2030 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 8618076 Dec. 11, 2030 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8618076 Dec. 11, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 8618076 Dec. 11, 2030 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 9393256 Sept. 14, 2032 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 9393256 Sept. 14, 2032 FOR THE TREATMENT OF HEPATITIS C
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 9393256 Sept. 14, 2032 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL 9393256 Sept. 14, 2032 FOR THE TREATMENT OF HEPATITIS C
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL 10039779 Jan. 30, 2034 FOR THE TREATMENT OF HEPATITIS C
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 10039779 Jan. 30, 2034 FOR THE TREATMENT OF GENOTYPE 1, 4, 5 OR 6 CHRONIC HEPATITIS C VIRUS (HCV) INFECTION
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL 10039779 Jan. 30, 2034 FOR TREATMENT-NAIVE GENOTYPE 1 PATIENTS WITH CHRONIC HEPATITIS C VIRUS (HCV) INFECTION FOR A DURATION OF 8-WEEKS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL Nov. 15, 2022 INFORMATION ADDED TO THE DOSING SECTION IN REGARD TO THE TREATMENT OF CHRONIC HEPATITIS C VIRUS INFECTION IN PATIENTS WITH SEVERE RENAL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENAL DISEASE ON DIALYSIS
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL Nov. 15, 2022 INFORMATION ADDED TO THE DOSING SECTION IN REGARD TO THE TREATMENT OF CHRONIC HEPATITIS C VIRUS INFECTION IN PATIENTS WITH SEVERE RENAL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENAL DISEASE ON DIALYSIS
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL Nov. 15, 2022 INFORMATION ADDED TO THE DOSING SECTION IN REGARD TO THE TREATMENT OF CHRONIC HEPATITIS C VIRUS INFECTION IN PATIENTS WITH SEVERE RENAL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENAL DISEASE ON DIALYSIS
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL Nov. 15, 2022 INFORMATION ADDED TO THE DOSING SECTION IN REGARD TO THE TREATMENT OF CHRONIC HEPATITIS C VIRUS INFECTION IN PATIENTS WITH SEVERE RENAL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENAL DISEASE ON DIALYSIS
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL April 7, 2024 FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL April 7, 2024 TREATMENT OF PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER OR WEIGHING AT LEAST 35 KG WITH CHRONIC HEPATITIS C VIRUS GENOTYPE 1, 4, 5, OR 6 INFECTION WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL Oct. 7, 2024 PEDIATRIC EXCLUSIVITY
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL Oct. 7, 2024 PEDIATRIC EXCLUSIVITY
45MG;200MG HARVONI GILEAD SCIENCES INC N205834 Aug. 28, 2019 RX TABLET ORAL Aug. 28, 2026 FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
90MG;400MG HARVONI GILEAD SCIENCES INC N205834 Oct. 10, 2014 RX TABLET ORAL Aug. 28, 2026 FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL Aug. 28, 2026 TREATMENT OF PEDIATRIC PATIENTS 3 YEARS OF AGE AND OLDER WITH CHRONIC HCV GENOTYPE 1 INFECTION WITH DECOMPENSATED CIRRHOSIS, FOR USE IN COMBINATION WITH RIBAVIRIN
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL Aug. 28, 2026 TREATMENT OF PEDIATRIC PATIENTS 3 YEARS OF AGE AND OLDER WITH CHRONIC HCV GENOTYPE 1 OR 4 INFECTION WHO ARE LIVER TRANSPLANT RECIPIENTS WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS, FOR USE IN COMBINATION WITH RIBAVIRIN
33.75MG;150MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL Aug. 28, 2026 TREATMENT OF PEDIATRIC PATIENTS BETWEEN 3 YEARS OF AGE AND 12 YEARS OF AGE OR WEIGHING 35 KG WITH CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 4, 5, OR 6 INFECTION WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL Aug. 28, 2026 TREATMENT OF PEDIATRIC PATIENTS 3 YEARS OF AGE AND OLDER WITH CHRONIC HCV GENOTYPE 1 INFECTION WITH DECOMPENSATED CIRRHOSIS, FOR USE IN COMBINATION WITH RIBAVIRIN
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL Aug. 28, 2026 TREATMENT OF PEDIATRIC PATIENTS 3 YEARS OF AGE AND OLDER WITH CHRONIC HCV GENOTYPE 1 OR 4 INFECTION WHO ARE LIVER TRANSPLANT RECIPIENTS WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS, FOR USE IN COMBINATION WITH RIBAVIRIN
45MG;200MG/PACKET HARVONI GILEAD SCIENCES INC N212477 Aug. 28, 2019 RX PELLETS ORAL Aug. 28, 2026 TREATMENT OF PEDIATRIC PATIENTS BETWEEN 3 YEARS OF AGE AND 12 YEARS OF AGE OR WEIGHING 35 KG WITH CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1, 4, 5, OR 6 INFECTION WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Genome polyprotein Polyprotein INHIBITOR EC50 11.40 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Genome polyprotein Polyprotein INHIBITOR EC50 10.51 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Nonstructural protein 5A Unclassified EC50 10.51 CHEMBL

External reference:

IDSource
013TE6E4WV UNII
D10442 KEGG_DRUG
4033796 VUID
N0000191095 NUI
4033796 VANDF
C3851350 UMLSCUI
CHEBI:85089 CHEBI
CHEMBL2374220 ChEMBL_ID
67505836 PUBCHEM_CID
DB09027 DRUGBANK_ID
C586541 MESH_SUPPLEMENTAL_RECORD_UI
11271 IUPHAR_LIGAND_ID
9796 INN_ID
1591922 RXNORM
30602 MMSL
d08295 MMSL
015709 NDDF
712517005 SNOMEDCT_US
714387002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Harvoni HUMAN PRESCRIPTION DRUG LABEL 2 61958-1801 TABLET, FILM COATED 90 mg ORAL NDA 36 sections
Harvoni Access HUMAN PRESCRIPTION DRUG LABEL 2 61958-1802 TABLET, FILM COATED 90 mg ORAL Export only 31 sections
Harvoni HUMAN PRESCRIPTION DRUG LABEL 2 61958-1803 TABLET, FILM COATED 45 mg ORAL NDA 36 sections
Harvoni HUMAN PRESCRIPTION DRUG LABEL 2 61958-1804 PELLET 45 mg ORAL NDA 36 sections
Harvoni HUMAN PRESCRIPTION DRUG LABEL 2 61958-1805 PELLET 33.75 mg ORAL NDA 36 sections
Ledipasvir and Sofosbuvir HUMAN PRESCRIPTION DRUG LABEL 2 72626-2601 TABLET, FILM COATED 90 mg ORAL NDA AUTHORIZED GENERIC 35 sections