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

Stem definitionDrug idCAS RN
antivirals RNA polymerase (NS5B) inhibitors 4811 1190307-88-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sofosbuvir
  • sovaldi
  • PSI-7977
A uridine monophosphate analog inhibitor of HEPATITIS C VIRUS (HCV) polymerase NS5B that is used as an ANTIVIRAL AGENT in the treatment of CHRONIC HEPATITIS C.
  • Molecular weight: 529.46
  • Formula: C22H29FN3O9P
  • CLOGP: 0.84
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 3
  • TPSA: 152.73
  • ALOGS: -2.81
  • ROTB: 11

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
0.40 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Hosey CM, Chan R, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Dec. 6, 2013 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 2717.35 16.84 2375 29714 475977 46177996
Fatigue 2476.06 16.84 2510 29579 606187 46047786
Hepatitis C 1729.95 16.84 468 31621 5850 46648123
Hepatocellular carcinoma 1335.93 16.84 324 31765 2515 46651458
Insomnia 427.06 16.84 545 31544 164379 46489594
Nausea 411.86 16.84 1213 30876 686241 45967732
Genotype drug resistance test positive 364.99 16.84 83 32006 467 46653506
Hepatic encephalopathy 326.66 16.84 153 31936 10004 46643969
Ascites 250.81 16.84 205 31884 36379 46617594
Hepatitis B reactivation 229.94 16.84 71 32018 1443 46652530
Product dose omission issue 212.83 16.84 400 31689 168120 46485853
Hepatic cirrhosis 211.82 16.84 133 31956 15599 46638374
Hepatitis C virus test positive 196.63 16.84 41 32048 141 46653832
Oesophageal varices haemorrhage 184.24 16.84 57 32032 1166 46652807
Anaemia 160.50 16.84 461 31628 255318 46398655
Treatment failure 148.45 16.84 245 31844 92842 46561131
Hepatic cancer recurrent 130.93 16.84 24 32065 31 46653942
Hepatic failure 130.84 16.84 137 31952 33279 46620694
Rheumatoid arthritis 127.44 16.84 10 32079 240205 46413768
Drug hypersensitivity 114.37 16.84 16 32073 243809 46410164
Hepatitis C RNULL positive 113.19 16.84 23 32066 67 46653906
Dyspepsia 108.80 16.84 180 31909 68292 46585681
Product use complaint 100.04 16.84 40 32049 1772 46652201
Toxicity to various agents 96.73 16.84 15 32074 211751 46442222
Liver transplant 95.35 16.84 42 32047 2375 46651598
Cryoglobulinaemia 94.57 16.84 26 32063 344 46653629
Viral load increased 88.78 16.84 34 32055 1341 46652632
Hyperbilirubinaemia 83.28 16.84 64 32025 10374 46643599
Drug intolerance 81.18 16.84 5 32084 147044 46506929
Diarrhoea 78.93 16.84 654 31435 558948 46095025
Hepatic cancer 76.56 16.84 39 32050 3058 46650915
Portal vein thrombosis 75.71 16.84 36 32053 2431 46651542
Irritability 75.08 16.84 96 31993 28850 46625123
Influenza like illness 69.16 16.84 134 31955 57436 46596537
Viral mutation identified 68.51 16.84 31 32058 1868 46652105
Pruritus 58.52 16.84 324 31765 242028 46411945
Maternal exposure during pregnancy 57.56 16.84 178 31911 102371 46551602
Renal impairment 56.39 16.84 144 31945 74228 46579745
Injection site pain 55.27 16.84 5 32084 107147 46546826
Intentional dose omission 55.07 16.84 32 32057 3258 46650715
Hepatitis C RNULL increased 54.50 16.84 14 32075 140 46653833
Exposure via body fluid 53.81 16.84 18 32071 476 46653497
Jaundice 50.09 16.84 79 32010 28766 46625207
Photosensitivity reaction 47.48 16.84 51 32038 12741 46641232
Product use in unapproved indication 47.13 16.84 4 32085 90269 46563704
Blood bilirubin increased 45.30 16.84 83 32006 34101 46619872
Disease progression 45.16 16.84 5 32084 91295 46562678
Varices oesophageal 43.46 16.84 26 32063 2793 46651180
Glomerular filtration rate decreased 42.31 16.84 46 32043 11648 46642325
Therapeutic product effect incomplete 42.10 16.84 3 32086 78150 46575823
Alopecia 41.75 16.84 221 31868 162193 46491780
Therapeutic product effect decreased 39.67 16.84 5 32084 82596 46571377
Hepatorenal syndrome 39.62 16.84 21 32068 1787 46652186
Fall 38.58 16.84 108 31981 328989 46324984
Dry skin 35.95 16.84 84 32005 40932 46613041
Depression 35.53 16.84 219 31870 169885 46484088
Myalgia 35.48 16.84 173 31916 122915 46531058
Hypotension 33.87 16.84 68 32021 232521 46421452
Systemic lupus erythematosus 33.72 16.84 3 32086 65177 46588796
Hepatic pain 33.62 16.84 22 32067 2766 46651207
Intentional overdose 33.57 16.84 3 32086 64941 46589032
Malignant neoplasm progression 33.55 16.84 3 32086 64923 46589050
Deep vein thrombosis 33.46 16.84 7 32082 79766 46574207
Sunburn 33.20 16.84 21 32068 2491 46651482
Arthropathy 32.45 16.84 9 32080 84691 46569282
Injection site erythema 32.33 16.84 6 32083 74421 46579552
Contraindicated product administered 31.57 16.84 8 32081 79939 46574034
Exposure via partner 31.45 16.84 9 32080 139 46653834
Musculoskeletal stiffness 31.41 16.84 14 32075 97979 46555994
Gastric varices haemorrhage 29.66 16.84 8 32081 98 46653875
Joint swelling 29.25 16.84 43 32046 166030 46487943
Ammonia increased 28.85 16.84 24 32065 4353 46649620
Infection 28.32 16.84 30 32059 133562 46520411
Peritonitis bacterial 27.81 16.84 32 32057 8621 46645352
Blood bilirubin abnormal 27.37 16.84 12 32077 671 46653302
Autoimmune hepatitis 26.99 16.84 30 32059 7784 46646189
Hepatectomy 26.98 16.84 7 32082 73 46653900
Osteoarthritis 26.94 16.84 5 32084 62020 46591953
Encephalopathy 26.44 16.84 66 32023 33523 46620450
Pain 26.35 16.84 206 31883 476742 46177231
Memory impairment 26.19 16.84 114 31975 77223 46576750
Remission not achieved 25.65 16.84 7 32082 90 46653883
Psoriasis 25.55 16.84 11 32078 78593 46575380
Condition aggravated 25.41 16.84 85 32004 244967 46409006
Extra dose administered 25.35 16.84 23 32066 4684 46649289
Asthenia 24.67 16.84 324 31765 310751 46343222
Hypersensitivity 24.49 16.84 41 32048 150280 46503693
Virologic failure 24.25 16.84 16 32073 2039 46651934
Constipation 24.06 16.84 203 31886 173894 46480079
C-reactive protein increased 22.87 16.84 6 32083 58584 46595389
Pneumonia 21.96 16.84 160 31929 376160 46277813
Rash 21.83 16.84 355 31734 356157 46297816
Hepatitis B 21.79 16.84 19 32070 3674 46650299
Abdominal distension 21.77 16.84 104 31985 73247 46580726
Chronic hepatitis C 21.37 16.84 7 32082 173 46653800
Pulmonary embolism 21.25 16.84 26 32063 108559 46545414
Decreased appetite 21.23 16.84 215 31874 193621 46460352
Swelling 21.18 16.84 33 32056 124478 46529495
Dizziness 20.84 16.84 339 31750 340075 46313898
Lower respiratory tract infection 20.83 16.84 6 32083 55083 46598890
Neutropenia 20.71 16.84 42 32047 143162 46510811
Chromaturia 20.57 16.84 37 32052 14982 46638991
Thirst 20.36 16.84 31 32058 10945 46643028
Drug interaction 20.23 16.84 221 31868 202873 46451100
Haemoglobin decreased 19.23 16.84 153 31936 128796 46525177
Gait disturbance 19.03 16.84 45 32044 145218 46508755
Inflammation 19.03 16.84 5 32084 48776 46605197
Emotional disorder 19.01 16.84 32 32057 12292 46641681
Hepatitis C RNULL 18.85 16.84 3 32086 0 46653973
Transcatheter arterial chemoembolisation 18.85 16.84 3 32086 0 46653973
Therapy cessation 18.57 16.84 50 32039 26579 46627394
Vomiting 18.22 16.84 423 31666 452371 46201602
Wrong schedule 18.14 16.84 6 32083 153 46653820
Sinusitis 17.97 16.84 39 32050 129729 46524244
Glomerulonephritis 17.97 16.84 12 32077 1561 46652412
Injection site pruritus 17.70 16.84 3 32086 39740 46614233
Chronic hepatic failure 17.62 16.84 8 32081 486 46653487
Hypoxia 17.25 16.84 7 32082 51831 46602142
Migraine 17.08 16.84 94 31995 69932 46584041

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
Hepatitis C 5568.59 15.27 1641 45752 11564 29893521
Fatigue 4247.21 15.27 3689 43704 316984 29588101
Headache 3936.85 15.27 2807 44586 179499 29725586
Hepatocellular carcinoma 2812.58 15.27 904 46489 8706 29896379
Treatment failure 1654.83 15.27 891 46502 33788 29871297
Genotype drug resistance test positive 1268.46 15.27 327 47066 1262 29903823
Drug ineffective 1056.40 15.27 1902 45491 338485 29566600
Insomnia 603.98 15.27 740 46653 92596 29812489
Hepatic cirrhosis 543.64 15.27 330 47063 15669 29889416
Liver transplant 425.64 15.27 162 47231 2640 29902445
Ascites 390.44 15.27 375 47018 35546 29869539
Hepatic encephalopathy 375.48 15.27 250 47143 13942 29891143
Nausea 359.62 15.27 1156 46237 295801 29609284
Product dose omission issue 358.61 15.27 571 46822 91060 29814025
Hepatitis C virus test positive 302.00 15.27 81 47312 376 29904709
Hepatic cancer 242.90 15.27 143 47250 6405 29898680
Viral mutation identified 241.61 15.27 106 47287 2520 29902565
Oesophageal varices haemorrhage 226.38 15.27 106 47287 2945 29902140
Intentional dose omission 218.61 15.27 83 47310 1342 29903743
Hepatitis B reactivation 201.32 15.27 96 47297 2781 29902304
Hepatic cancer recurrent 182.48 15.27 52 47341 314 29904771
Toxicity to various agents 181.75 15.27 31 47362 177152 29727933
Hepatitis C RNULL positive 181.45 15.27 47 47346 185 29904900
Hepatic failure 177.34 15.27 243 47150 33800 29871285
Hypotension 158.11 15.27 60 47333 200505 29704580
Dyspepsia 142.38 15.27 206 47187 30123 29874962
Irritability 125.26 15.27 168 47225 22882 29882203
Hepatitis C RNULL increased 116.23 15.27 37 47356 341 29904744
Febrile neutropenia 113.04 15.27 17 47376 106676 29798409
Pneumonia 108.36 15.27 230 47163 334076 29571009
Hepatorenal syndrome 104.19 15.27 59 47334 2452 29902633
Virologic failure 103.11 15.27 64 47329 3155 29901930
Chronic hepatitis C 98.44 15.27 35 47358 465 29904620
Hyperbilirubinaemia 95.91 15.27 126 47267 16816 29888269
Influenza like illness 90.95 15.27 153 47240 25452 29879633
Hepatic hydrothorax 87.22 15.27 19 47374 26 29905059
Abdominal discomfort 86.76 15.27 219 47174 48572 29856513
Malignant neoplasm progression 85.22 15.27 8 47385 72279 29832806
Portal vein thrombosis 79.66 15.27 56 47337 3408 29901677
Bleeding varicose vein 77.89 15.27 26 47367 282 29904803
Blood bilirubin increased 76.47 15.27 175 47218 36461 29868624
Drug abuse 74.47 15.27 19 47374 82053 29823032
Completed suicide 69.96 15.27 35 47358 99457 29805628
Drug hypersensitivity 67.94 15.27 13 47380 68506 29836579
General physical health deterioration 67.55 15.27 37 47356 99907 29805178
Diarrhoea 66.88 15.27 814 46579 333289 29571796
Varices oesophageal 65.47 15.27 50 47343 3459 29901626
Anaemia 65.22 15.27 556 46837 207436 29697649
Tachycardia 65.14 15.27 18 47375 73721 29831364
Fall 64.88 15.27 118 47275 181754 29723331
Viral load increased 60.70 15.27 44 47349 2810 29902275
Glomerular filtration rate decreased 60.46 15.27 82 47311 11280 29893805
Pyrexia 60.17 15.27 251 47142 294238 29610847
Jaundice 57.91 15.27 146 47247 32340 29872745
Pulmonary embolism 55.65 15.27 27 47366 78108 29826977
Disease progression 54.79 15.27 29 47364 79845 29825240
Peritonitis bacterial 54.40 15.27 78 47315 11300 29893785
Neutropenia 53.74 15.27 75 47318 128465 29776620
Plasma cell myeloma 53.30 15.27 10 47383 53452 29851633
Product use in unapproved indication 51.67 15.27 26 47367 73667 29831418
Ammonia abnormal 50.85 15.27 14 47379 73 29905012
Oxygen saturation decreased 50.67 15.27 5 47388 43435 29861650
Depression 50.58 15.27 279 47114 90158 29814927
Dyspnoea 50.00 15.27 316 47077 332979 29572106
Cardiac failure congestive 49.16 15.27 37 47356 84370 29820715
Therapeutic embolisation 49.16 15.27 19 47374 323 29904762
Product use complaint 47.61 15.27 27 47366 1125 29903960
Therapy cessation 46.66 15.27 85 47308 15052 29890033
Respiratory failure 44.83 15.27 56 47337 100586 29804499
Hepatic pain 44.62 15.27 27 47366 1271 29903814
Coronary artery disease 44.14 15.27 12 47381 49700 29855385
Cryoglobulinaemia 43.09 15.27 17 47376 306 29904779
Abnormal dreams 42.32 15.27 58 47335 8057 29897028
Pruritus 41.26 15.27 324 47069 117880 29787205
Interstitial lung disease 41.07 15.27 22 47371 60175 29844910
Extra dose administered 40.86 15.27 35 47358 2851 29902234
Incorrect product administration duration 40.75 15.27 40 47353 3882 29901203
White blood cell count decreased 40.30 15.27 44 47349 83903 29821182
Dry skin 40.10 15.27 101 47292 22353 29882732
Therapeutic product effect incomplete 39.18 15.27 4 47389 33830 29871255
Asthma 37.73 15.27 6 47387 36168 29868917
Gait disturbance 37.23 15.27 38 47355 74739 29830346
Hyponatraemia 37.18 15.27 31 47362 67171 29837914
Hypoxia 36.47 15.27 15 47378 47839 29857246
Rheumatoid arthritis 36.47 15.27 10 47383 41187 29863898
Neutrophil count decreased 36.30 15.27 11 47382 42443 29862642
C-reactive protein increased 35.87 15.27 12 47381 43461 29861624
Respiratory arrest 35.11 15.27 3 47390 29255 29875830
Therapeutic product effect decreased 34.84 15.27 3 47390 29073 29876012
Deep vein thrombosis 34.61 15.27 27 47366 60474 29844611
Haematuria 34.26 15.27 14 47379 44820 29860265
Remission not achieved 34.07 15.27 10 47383 68 29905017
Focal segmental glomerulosclerosis 34.01 15.27 26 47367 1801 29903284
Sepsis 33.51 15.27 119 47274 146276 29758809
Pancytopenia 33.20 15.27 52 47341 85000 29820085
Myalgia 32.98 15.27 221 47172 76446 29828639
Atrial fibrillation 32.70 15.27 77 47316 108047 29797038
Neuropathy peripheral 32.66 15.27 38 47355 70437 29834648
Gastric varices haemorrhage 32.50 15.27 13 47380 243 29904842
Complications of transplanted lung 32.48 15.27 12 47381 179 29904906
Gene mutation identification test positive 32.24 15.27 12 47381 183 29904902
Encephalopathy 32.09 15.27 118 47275 32087 29872998
Dry mouth 32.01 15.27 94 47299 22756 29882329
Hypokalaemia 31.88 15.27 20 47373 50172 29854913
Platelet count decreased 31.76 15.27 76 47317 106053 29799032
Cardiac failure 31.62 15.27 52 47341 83366 29821719
Pulmonary oedema 31.60 15.27 15 47378 43960 29861125
Erythema 31.54 15.27 46 47347 77405 29827680
Blood pressure decreased 30.96 15.27 18 47375 47057 29858028
International normalised ratio increased 30.35 15.27 19 47374 47720 29857365
Alpha 1 foetoprotein increased 30.20 15.27 17 47376 698 29904387
Hepatic mass 29.66 15.27 19 47374 990 29904095
Electrocardiogram QT prolonged 29.37 15.27 10 47383 35825 29869260
Hepatic neoplasm 29.33 15.27 24 47369 1835 29903250
Dehydration 29.22 15.27 99 47294 123440 29781645
Drug reaction with eosinophilia and systemic symptoms 29.10 15.27 5 47388 28483 29876602
Intentional overdose 28.52 15.27 15 47378 41466 29863619
Genital herpes simplex 28.46 15.27 10 47383 128 29904957
Treatment noncompliance 28.14 15.27 96 47297 25157 29879928
Photosensitivity reaction 28.07 15.27 53 47340 9641 29895444
Ammonia increased 27.89 15.27 34 47359 4207 29900878
Energy increased 27.89 15.27 20 47373 1256 29903829
Injection site pain 27.51 15.27 7 47386 30303 29874782
Flushing 26.40 15.27 7 47386 29485 29875600
Depressed level of consciousness 26.02 15.27 14 47379 38208 29866877
Coma 25.85 15.27 16 47377 40433 29864652
Urinary retention 25.60 15.27 10 47383 32907 29872178
Accidental overdose 25.42 15.27 75 47318 18200 29886885
Cholangiocarcinoma 25.28 15.27 17 47376 962 29904123
Porphyria non-acute 24.43 15.27 13 47380 477 29904608
Cardiac arrest 24.35 15.27 71 47322 92779 29812306
Mobility decreased 23.60 15.27 6 47387 25993 29879092
Hypocalcaemia 23.57 15.27 3 47390 21373 29883712
Stomatitis 23.47 15.27 15 47378 37264 29867821
Anticoagulation drug level below therapeutic 23.29 15.27 14 47379 651 29904434
Genital herpes 23.11 15.27 13 47380 533 29904552
Ectopic kidney 23.09 15.27 7 47386 54 29905031
Thrombocytopenia 23.07 15.27 125 47268 136919 29768166
Biliary colic 22.55 15.27 16 47377 988 29904097
Cardio-respiratory arrest 22.39 15.27 35 47358 57271 29847814
Hepatitis C RNULL 22.34 15.27 6 47387 28 29905057
Liver transplant rejection 22.06 15.27 22 47371 2176 29902909
Diabetic hyperglycaemic coma 21.68 15.27 6 47387 32 29905053
Thought blocking 21.49 15.27 8 47385 122 29904963
Hepatectomy 21.48 15.27 7 47386 70 29905015
Tinnitus 21.41 15.27 65 47328 16023 29889062
Chronic obstructive pulmonary disease 21.22 15.27 25 47368 46101 29858984
Migraine 21.02 15.27 56 47337 12818 29892267
Abdominal pain upper 20.99 15.27 170 47223 62381 29842704
Memory impairment 20.96 15.27 115 47278 37059 29868026
Hepatic fibrosis 20.83 15.27 27 47366 3553 29901532
Bronchitis 20.48 15.27 19 47374 39106 29865979
Intentional product misuse 20.42 15.27 15 47378 34652 29870433
Portal hypertensive gastropathy 20.30 15.27 12 47381 541 29904544
Acute respiratory distress syndrome 20.21 15.27 6 47387 23466 29881619
Pneumonia aspiration 20.19 15.27 18 47375 37762 29867323
Wheezing 20.10 15.27 12 47381 30926 29874159
Hunger 20.07 15.27 17 47376 1363 29903722
Pain in extremity 19.98 15.27 98 47295 110123 29794962
Adverse drug reaction 19.78 15.27 6 47387 23139 29881946
Blood bilirubin abnormal 19.36 15.27 12 47381 590 29904495
Abdominal cavity drainage 19.33 15.27 10 47383 346 29904739
Acute kidney injury 19.32 15.27 311 47082 273531 29631554
Staphylococcal infection 19.25 15.27 12 47381 30212 29874873
Tumour embolism 19.17 15.27 6 47387 52 29905033
Portal hypertension 19.17 15.27 27 47366 3846 29901239
Urticaria 18.91 15.27 36 47357 54570 29850515
Laryngomalacia 18.79 15.27 9 47384 263 29904822
Delirium 18.72 15.27 22 47371 40609 29864476
Serotonin syndrome 18.58 15.27 3 47390 17888 29887197
Respiratory distress 18.49 15.27 15 47378 32957 29872128
Drug intolerance 18.33 15.27 27 47366 45264 29859821
Haematemesis 18.23 15.27 86 47307 26117 29878968
Seizure 18.17 15.27 87 47306 98388 29806697
Urinary tract infection 18.11 15.27 58 47335 73601 29831484
Lymphocyte count decreased 18.08 15.27 4 47389 19051 29886034
Foetal exposure during pregnancy 18.04 15.27 19 47374 36852 29868233
Acute on chronic liver failure 17.74 15.27 7 47386 126 29904959
Gallbladder cancer 17.53 15.27 8 47385 209 29904876
Hydrocholecystis 17.53 15.27 8 47385 209 29904876
Prostate cancer 17.47 15.27 8 47385 23949 29881136
Viral test positive 17.22 15.27 8 47385 218 29904867
Rhabdomyolysis 17.11 15.27 48 47345 63532 29841553
Gastrointestinal tube insertion 17.05 15.27 15 47378 1266 29903819
Coma hepatic 16.97 15.27 10 47383 448 29904637
Hyperkalaemia 16.92 15.27 51 47342 65959 29839126
Eosinophilia 16.79 15.27 7 47386 22153 29882932
Neoplasm progression 16.67 15.27 4 47389 18019 29887066
Increased appetite 16.62 15.27 31 47362 5586 29899499
Anaphylactic reaction 16.62 15.27 12 47381 27970 29877115
Therapeutic response decreased 16.45 15.27 9 47384 24340 29880745
Pleural effusion 16.40 15.27 61 47332 74005 29831080
Unresponsive to stimuli 16.13 15.27 11 47382 26408 29878677
Pneumonitis 16.01 15.27 12 47381 27442 29877643
Respiratory disorder 15.95 15.27 4 47389 17490 29887595
Loss of consciousness 15.91 15.27 68 47325 79307 29825778
Hypersensitivity 15.90 15.27 39 47354 53989 29851096
Myelodysplastic syndrome 15.81 15.27 5 47388 18773 29886312
Pulmonary fibrosis 15.77 15.27 3 47390 15887 29889198
Gastrooesophageal reflux disease 15.71 15.27 96 47297 32159 29872926
Gastric varices 15.65 15.27 9 47384 385 29904700
Hypoglycaemia 15.64 15.27 36 47357 50945 29854140
Product packaging quantity issue 15.42 15.27 11 47382 685 29904400
Pallor 15.39 15.27 7 47386 21042 29884043
Haemophilia 15.39 15.27 4 47389 16 29905069
Myocardial infarction 15.39 15.27 126 47267 125499 29779586

Pharmacologic Action:

SourceCodeDescription
ATC J05AP08 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
ATC J05AP51 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
ATC J05AP55 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
ATC J05AP56 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
FDA EXT N0000175459 Nucleoside Analog
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
FDA MoA N0000191258 RNULL Replicase Inhibitors
FDA EPC N0000191493 Hepatitis C Virus Nucleotide Analog NS5B Polymerase Inhibitor
CHEBI has role CHEBI:36044 anti-virus drug
CHEBI has role CHEBI:50266 prodrugs
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 9.07 acidic
pKa2 11.58 acidic
pKa3 2.07 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL June 28, 2021 NEW CHEMICAL ENTITY
400MG;100MG;100MG VOSEVI GILEAD SCIENCES INC N209195 July 18, 2017 RX TABLET ORAL July 18, 2022 NEW CHEMICAL ENTITY
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 RENULLL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENULLL 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 RENULLL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENULLL DISEASE ON DIALYSIS
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 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 RENULLL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENULLL 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 RENULLL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENULLL 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 RENULLL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENULLL DISEASE ON DIALYSIS
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL March 19, 2023 NEW STRENGTH
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL March 19, 2023 NEW PATIENT POPULATION
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL May 15, 2023 PEDIATRIC EXCLUSIVITY
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL July 14, 2023 INFORMATION ADDED TO THE LABELING DESCRIBING A PHASE 2, MULTICENTER, OPEN-LABEL STUDY TO EVALUATE THE SAFETY/EFFICACY OF SOFOSBUVIR/VELPATASVIR IN SUBJECTS WITH CHRONIC HCV INFECTION WHO HAVE RECEIVED A LIVER TRANSPLANT
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL July 14, 2023 INFORMATION ADDED TO THE LABELING DESCRIBING A PHASE 2, MULTICENTER, OPEN-LABEL STUDY TO EVALUATE THE SAFETY/EFFICACY OF SOFOSBUVIR/VELPATASVIR IN SUBJECTS WITH CHRONIC HCV INFECTION WHO HAVE RECEIVED A LIVER TRANSPLANT
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL Sept. 19, 2023 PEDIATRIC EXCLUSIVITY
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL Sept. 19, 2023 PEDIATRIC EXCLUSIVITY
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL Jan. 14, 2024 PEDIATRIC EXCLUSIVITY
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL Jan. 14, 2024 PEDIATRIC EXCLUSIVITY
200MG SOVALDI GILEAD SCIENCES INC N204671 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)
400MG SOVALDI GILEAD SCIENCES INC N204671 Dec. 6, 2013 RX TABLET ORAL April 7, 2024 TREATMENT OF CHRONIC HCV GENOTYPE 2 OR 3 INFECTION IN PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER OR WEIGHING AT LEAST 35 KG WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS FOR USE IN COMBINULLTION WITH RIBAVIRIN
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
200MG SOVALDI GILEAD SCIENCES INC N204671 Aug. 28, 2019 RX TABLET ORAL Oct. 7, 2024 PEDIATRIC EXCLUSIVITY
400MG SOVALDI GILEAD SCIENCES INC N204671 Dec. 6, 2013 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
200MG SOVALDI GILEAD SCIENCES INC N204671 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)
400MG SOVALDI GILEAD SCIENCES INC N204671 Dec. 6, 2013 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 COMBINULLTION 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 COMBINULLTION 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 COMBINULLTION 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 COMBINULLTION 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
150MG/PACKET SOVALDI GILEAD SCIENCES INC N212480 Aug. 28, 2019 RX PELLETS ORAL Aug. 28, 2026 FOR THE TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 2 OR 3 INFECTION IN PEDIATRIC PATIENTS BETWEEN 3 YEARS OF AGE AND 12 YEARS OF AGE OR WEIGHING 35 KG WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS FOR USE IN COMBINULLTION WITH RIBAVIRIN
200MG/PACKET SOVALDI GILEAD SCIENCES INC N212480 Aug. 28, 2019 RX PELLETS ORAL Aug. 28, 2026 FOR THE TREATMENT OF CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 2 OR 3 INFECTION IN PEDIATRIC PATIENTS BETWEEN 3 YEARS OF AGE AND 12 YEARS OF AGE OR WEIGHING 35 KG WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS FOR USE IN COMBINULLTION WITH RIBAVIRIN
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL March 19, 2027 TX OF PED PTS 6 YRS OF AGE & OLDER OR WEIGHING AT LEAST 17 KG WITH CHRONIC HEPATITIS C VIRUS GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION: WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS; OR WITH DECOMPENSATED CIRRHOSIS FOR USE IN COMBINULLTION WITH RIBAVIRIN
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL March 19, 2027 TX OF PED PTS 6 YRS OF AGE & OLDER OR WEIGHING AT LEAST 17 KG WITH CHRONIC HEPATITIS C VIRUS GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION: WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS; OR WITH DECOMPENSATED CIRRHOSIS FOR USE IN COMBINULLTION WITH RIBAVIRIN
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL Sept. 19, 2027 PEDIATRIC EXCLUSIVITY
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL Sept. 19, 2027 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Genome polyprotein Polyprotein INHIBITOR EC90 6.96 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
NS5B protein Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
D10366 KEGG_DRUG
4032949 VUID
N0000189539 NUI
4032949 VANDF
C2976303 UMLSCUI
CHEBI:85083 CHEBI
CHEMBL1259059 ChEMBL_ID
D000069474 MESH_DESCRIPTOR_UI
7368 IUPHAR_LIGAND_ID
9665 INN_ID
DB08934 DRUGBANK_ID
WJ6CA3ZU8B UNII
45375806 PUBCHEM_CID
11311503 PUBCHEM_CID
1484911 RXNORM
207812 MMSL
29932 MMSL
d08184 MMSL
015326 NDDF
710806008 SNOMEDCT_US
713645002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Sovaldi HUMAN PRESCRIPTION DRUG LABEL 1 61958-1501 TABLET, FILM COATED 400 mg ORAL NDA 34 sections
Sovaldi Access HUMAN PRESCRIPTION DRUG LABEL 1 61958-1502 TABLET, FILM COATED 400 mg ORAL Export only 34 sections
Sovaldi HUMAN PRESCRIPTION DRUG LABEL 1 61958-1503 TABLET, FILM COATED 200 mg ORAL NDA 34 sections
Sovaldi HUMAN PRESCRIPTION DRUG LABEL 1 61958-1504 PELLET 150 mg ORAL NDA 34 sections
Sovaldi HUMAN PRESCRIPTION DRUG LABEL 1 61958-1505 PELLET 200 mg ORAL NDA 34 sections
Harvoni HUMAN PRESCRIPTION DRUG LABEL 2 61958-1801 TABLET, FILM COATED 400 mg ORAL NDA 36 sections
Harvoni Access HUMAN PRESCRIPTION DRUG LABEL 2 61958-1802 TABLET, FILM COATED 400 mg ORAL Export only 31 sections
Harvoni HUMAN PRESCRIPTION DRUG LABEL 2 61958-1803 TABLET, FILM COATED 200 mg ORAL NDA 36 sections
Harvoni HUMAN PRESCRIPTION DRUG LABEL 2 61958-1804 PELLET 200 mg ORAL NDA 36 sections
Harvoni HUMAN PRESCRIPTION DRUG LABEL 2 61958-1805 PELLET 150 mg ORAL NDA 36 sections
Epclusa HUMAN PRESCRIPTION DRUG LABEL 2 61958-2201 TABLET, FILM COATED 400 mg ORAL NDA 36 sections
Epclusa Access HUMAN PRESCRIPTION DRUG LABEL 2 61958-2202 TABLET, FILM COATED 400 mg ORAL Export only 31 sections
Epclusa HUMAN PRESCRIPTION DRUG LABEL 2 61958-2203 TABLET, FILM COATED 200 mg ORAL NDA 36 sections
Epclusa HUMAN PRESCRIPTION DRUG LABEL 2 61958-2204 PELLET 200 mg ORAL NDA 36 sections
Epclusa HUMAN PRESCRIPTION DRUG LABEL 2 61958-2205 PELLET 150 mg ORAL NDA 36 sections
Vosevi HUMAN PRESCRIPTION DRUG LABEL 3 61958-2401 TABLET, FILM COATED 400 mg ORAL NDA 34 sections
Ledipasvir and Sofosbuvir HUMAN PRESCRIPTION DRUG LABEL 2 72626-2601 TABLET, FILM COATED 400 mg ORAL NDA AUTHORIZED GENERIC 35 sections
Sofosbuvir and Velpatasvir HUMAN PRESCRIPTION DRUG LABEL 2 72626-2701 TABLET, FILM COATED 400 mg ORAL NDA AUTHORIZED GENERIC 35 sections