darunavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
HIV protease inhibitors 4143 206361-99-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • darunavir
  • darunavir ethanolate
  • prezista
  • TMC-114
  • TMC 114
  • darunavir ethnolate
An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS. There was some evidence of in vitro activity against SARS-CoV-2, but no clinical trial data was found to support use in the treatment of COVID-19.
  • Molecular weight: 547.67
  • Formula: C27H37N3O7S
  • CLOGP: 2.89
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 3
  • TPSA: 140.42
  • ALOGS: -3.91
  • ROTB: 11
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.20 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.15 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1.20 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 20.87 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 37 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance) 7.81 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 15 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.516 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 6.353 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 38.194 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 15.101 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 17.180 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 29.370 % High 1
herg hERG pIC50 4.372 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 30.620 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 273.527 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 20.340 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK 23
kinase-selectivity-class GRK2,PDK1 2
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 20.845 Moderate 0.72
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 10.447 High 1
mh-clint Mouse hepatocyte intrinsic clearance 131.826 High 1
mppb Mouse plasma protein binding (% unbound) 13.460 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 52.602 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 24.700 % High 1
rat-kpuu-brain Rat brain Kpuu 0.015 % Moderate 0.72
rh-clint Rat hepatocyte intrinsic clearance 137.721 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 69.320 % High 1
rppb Rat plasma protein binding (% unbound) 17.350 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 233.884 uM High 1

Approvals:

DateAgencyCompanyOrphan
Feb. 12, 2007 EMA Janssen-Cilag International NV
June 23, 2006 FDA JANSSEN PRODS
Nov. 22, 2007 PMDA Janssen Pharmaceutical K.K.

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
Foetal exposure during pregnancy 963.21 28.22 303 9786 42672 90575686
Exposure during pregnancy 931.89 28.22 475 9614 237935 90380423
Abortion spontaneous 851.67 28.22 292 9797 53764 90564594
Maternal exposure during pregnancy 444.58 28.22 346 9743 359717 90258641
Virologic failure 348.32 28.22 74 10015 2150 90616208
Drug interaction 313.24 28.22 253 9836 276200 90342158
Premature labour 272.83 28.22 88 10001 13288 90605070
Premature baby 264.71 28.22 101 9988 24976 90593382
Premature delivery 238.17 28.22 106 9983 38656 90579702
Treatment noncompliance 232.69 28.22 114 9975 51613 90566745
Abortion induced 229.39 28.22 75 10014 11813 90606545
Viral mutation identified 198.98 28.22 46 10043 1979 90616379
Lipodystrophy acquired 179.03 28.22 40 10049 1474 90616884
Foetal growth restriction 172.19 28.22 57 10032 9323 90609035
Blood HIV RNA increased 167.27 28.22 34 10055 790 90617568
Viral load increased 167.09 28.22 38 10051 1518 90616840
Live birth 157.09 28.22 102 9987 79005 90539353
Immune reconstitution inflammatory syndrome 146.44 28.22 47 10042 6972 90611386
Pathogen resistance 139.74 28.22 47 10042 8068 90610290
Spina bifida 136.16 28.22 29 10060 851 90617507
Stillbirth 135.69 28.22 45 10044 7398 90610960
Premature rupture of membranes 131.64 28.22 41 10048 5517 90612841
Foetal death 131.48 28.22 58 10031 20665 90597693
Hepatocellular injury 112.99 28.22 58 10031 28900 90589458
Drug resistance 110.24 28.22 58 10031 30391 90587967
Supernumerary nipple 106.76 28.22 16 10073 51 90618307
Genotype drug resistance test positive 105.92 28.22 21 10068 428 90617930
Congenital naevus 103.47 28.22 18 10071 172 90618186
Low birth weight baby 102.96 28.22 39 10050 9428 90608930
Caesarean section 101.98 28.22 47 10042 18530 90599828
Acoustic stimulation tests abnormal 100.35 28.22 16 10073 84 90618274
Congenital genital malformation 98.35 28.22 17 10072 156 90618202
Cholestasis of pregnancy 94.23 28.22 24 10065 1553 90616805
Anal atresia 93.90 28.22 19 10070 431 90617927
Cloacal exstrophy 92.25 28.22 16 10073 150 90618208
Low set ears 90.11 28.22 17 10072 264 90618094
Bladder agenesis 86.16 28.22 15 10074 144 90618214
Genitalia external ambiguous 85.52 28.22 15 10074 151 90618207
Caudal regression syndrome 82.80 28.22 15 10074 184 90618174
Gastrointestinal disorder congenital 80.27 28.22 14 10075 136 90618222
Ectopic pregnancy 77.13 28.22 24 10065 3217 90615141
Tethered cord syndrome 76.96 28.22 15 10074 279 90618079
Gastrointestinal malformation 75.43 28.22 14 10075 198 90618160
Meconium stain 75.30 28.22 14 10075 200 90618158
CD4 lymphocytes decreased 75.29 28.22 20 10069 1527 90616831
Congenital heart valve disorder 74.05 28.22 12 10077 71 90618287
Meningomyelocele 70.66 28.22 16 10073 626 90617732
Pain 70.53 28.22 13 10076 996328 89622030
Sudden infant death syndrome 69.08 28.22 14 10075 320 90618038
Cerebral ventricle dilatation 67.85 28.22 17 10072 1029 90617329
Exomphalos 67.08 28.22 15 10074 554 90617804
Gastroschisis 65.95 28.22 14 10075 404 90617954
Gestational diabetes 65.12 28.22 29 10060 10553 90607805
Umbilical cord abnormality 64.38 28.22 15 10074 667 90617691
Congenital choroid plexus cyst 62.99 28.22 13 10076 326 90618032
Congenital pulmonary valve disorder 61.44 28.22 10 10079 61 90618297
Ventricular septal defect 61.42 28.22 23 10066 5384 90612974
Hydrocephalus 58.74 28.22 23 10066 6071 90612287
Rash maculo-papular 58.15 28.22 43 10046 40890 90577468
Pre-eclampsia 57.66 28.22 27 10062 11021 90607337
CSF HIV escape syndrome 57.16 28.22 10 10079 99 90618259
Coloboma 56.37 28.22 10 10079 108 90618250
Hemivertebra 55.48 28.22 10 10079 119 90618239
Cushingoid 53.01 28.22 25 10064 10370 90607988
Hyperadrenocorticism 52.79 28.22 12 10077 478 90617880
Fatigue 51.07 28.22 33 10056 1153990 89464368
Neural tube defect 50.71 28.22 10 10079 198 90618160
Foetal malnutrition 50.42 28.22 9 10080 101 90618257
Neonatal respiratory arrest 49.27 28.22 8 10081 48 90618310
Atrial septal defect 48.86 28.22 22 10067 8212 90610146
Nephropathy toxic 48.28 28.22 25 10064 12663 90605695
Maternal drugs affecting foetus 48.09 28.22 19 10070 5136 90613222
Foetal growth abnormality 47.72 28.22 8 10081 60 90618298
Eosinophilia 47.47 28.22 33 10056 28500 90589858
Hepatitis B DNA increased 47.40 28.22 10 10079 280 90618078
Ichthyosis 46.62 28.22 8 10081 70 90618288
Atrioventricular septal defect 45.49 28.22 10 10079 341 90618017
Complication of delivery 45.36 28.22 9 10080 184 90618174
Pulmonary valve sclerosis 44.89 28.22 7 10082 31 90618327
Amniotic cavity infection 44.71 28.22 13 10076 1383 90616975
Left ventricular dilatation 44.09 28.22 11 10078 654 90617704
Complication of pregnancy 43.46 28.22 11 10078 694 90617664
Lipohypertrophy 42.94 28.22 11 10078 728 90617630
Oligohydramnios 41.96 28.22 19 10070 7182 90611176
Hepatitis cholestatic 41.85 28.22 20 10069 8541 90609817
Renal tubular disorder 41.44 28.22 15 10074 3192 90615166
Congenital anomaly 41 28.22 18 10071 6329 90612029
Alopecia 40.75 28.22 4 10085 495067 90123291
Abortion of ectopic pregnancy 40.42 28.22 7 10082 65 90618293
Endometritis decidual 40.06 28.22 6 10083 19 90618339
Acute kidney injury 40.01 28.22 101 9988 320286 90298072
Psychomotor retardation 38.97 28.22 16 10073 4773 90613585
Cholestasis 38.30 28.22 32 10057 36267 90582091
Osteonecrosis 38.24 28.22 28 10061 26213 90592145
Congenital ectopic bladder 37.27 28.22 7 10082 106 90618252
Enzyme activity increased 37.05 28.22 5 10084 5 90618353
Fanconi syndrome acquired 37.01 28.22 11 10078 1263 90617095
Dermatitis exfoliative generalised 36.58 28.22 16 10073 5577 90612781
Hepatic cytolysis 36.28 28.22 29 10060 30887 90587471
Plagiocephaly 36.23 28.22 7 10082 124 90618234
Total bile acids increased 36.13 28.22 7 10082 126 90618232
Central obesity 36.06 28.22 11 10078 1379 90616979
Breast disorder 35.97 28.22 13 10076 2754 90615604
HIV-associated neurocognitive disorder 35.87 28.22 7 10082 131 90618227
Congenital anomaly in offspring 34.88 28.22 7 10082 152 90618206
Skin striae 34.60 28.22 11 10078 1580 90616778
Anencephaly 33.62 28.22 8 10081 390 90617968
Polyhydramnios 33.42 28.22 12 10077 2496 90615862
Ventricular hypertrophy 33.39 28.22 13 10076 3378 90614980
Potassium wasting nephropathy 33.16 28.22 6 10083 73 90618285
Immunosuppressant drug level increased 32.61 28.22 14 10075 4666 90613692
Fanconi syndrome 32.44 28.22 11 10078 1932 90616426
Generalised anxiety disorder 32.35 28.22 12 10077 2735 90615623
Congenital aortic valve incompetence 32.28 28.22 5 10084 21 90618337
Abortion 32.15 28.22 12 10077 2783 90615575
Abdominal discomfort 32.06 28.22 7 10082 477321 90141037
Drug ineffective 31.68 28.22 67 10022 1384231 89234127
Large for dates baby 31.51 28.22 8 10081 511 90617847
CSF test abnormal 31.19 28.22 8 10081 532 90617826
Eyelid oedema 30.83 28.22 18 10071 11516 90606842
Adrenal insufficiency 30.78 28.22 26 10063 29895 90588463
Arthralgia 30.78 28.22 25 10064 778497 89839861
Fall 30.52 28.22 8 10081 481802 90136556
Glucocorticoids increased 30.37 28.22 6 10083 120 90618238
Congenital absence of bile ducts 30.25 28.22 5 10084 34 90618324
Sepsis neonatal 30.19 28.22 8 10081 605 90617753
Heart disease congenital 30.17 28.22 10 10079 1639 90616719
Infection 29.59 28.22 3 10086 362091 90256267
Swelling 28.43 28.22 6 10083 419052 90199306
Maxillonasal dysplasia 28.37 28.22 4 10085 7 90618351
Foetal heart rate disorder 28.27 28.22 6 10083 173 90618185

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
Immune reconstitution inflammatory syndrome 594.96 15.59 205 17656 9938 42593536
Foetal exposure during pregnancy 531.61 15.59 298 17563 47013 42556461
Lipodystrophy acquired 456.77 15.59 130 17731 3320 42600154
Drug interaction 412.78 15.59 531 17330 266468 42337006
Virologic failure 352.40 15.59 110 17751 3884 42599590
Progressive external ophthalmoplegia 308.46 15.59 79 17782 1332 42602142
Mitochondrial toxicity 308.06 15.59 90 17771 2525 42600949
Eyelid ptosis 257.34 15.59 99 17762 6562 42596912
Blood HIV RNA increased 206.25 15.59 59 17802 1532 42601942
Viral mutation identified 205.58 15.59 70 17791 3261 42600213
Pathogen resistance 199.66 15.59 97 17764 11353 42592121
Osteoporosis 151.22 15.59 88 17773 14818 42588656
CD4 lymphocytes decreased 140.96 15.59 46 17815 1875 42601599
Viral load increased 131.85 15.59 49 17812 2948 42600526
Diplopia 130.93 15.59 90 17771 20226 42583248
Genotype drug resistance test positive 126.77 15.59 38 17823 1166 42602308
Drug resistance 126.60 15.59 109 17752 34139 42569335
Premature baby 122.59 15.59 91 17770 23062 42580412
HIV-associated neurocognitive disorder 108.93 15.59 26 17835 322 42603152
Renal tubular disorder 108.47 15.59 49 17812 4860 42598614
Dyslipidaemia 107.32 15.59 60 17801 9358 42594116
Laryngomalacia 104.49 15.59 25 17836 313 42603161
Syphilis 95.66 15.59 26 17835 556 42602918
Treatment noncompliance 89.67 15.59 94 17767 37578 42565896
Trisomy 21 81.83 15.59 23 17838 559 42602915
Osteonecrosis 80.94 15.59 61 17800 15804 42587670
Adrenal suppression 78.53 15.59 25 17836 940 42602534
Brain stem stroke 78.52 15.59 20 17841 329 42603145
Hypertriglyceridaemia 72.74 15.59 48 17813 10078 42593396
Gene mutation 70.65 15.59 27 17834 1754 42601720
Ophthalmoplegia 68.52 15.59 28 17833 2172 42601302
Polydactyly 64.82 15.59 23 17838 1211 42602263
Renal impairment 58.37 15.59 137 17724 110091 42493383
CSF HIV escape syndrome 57.20 15.59 14 17847 194 42603280
Fanconi syndrome acquired 56.57 15.59 24 17837 2046 42601428
Congenital hydronephrosis 54.11 15.59 18 17843 779 42602695
Mycobacterium avium complex infection 53.81 15.59 26 17835 3001 42600473
Hepatitis cholestatic 52.84 15.59 39 17822 9785 42593689
Ventricular hypoplasia 52.76 15.59 11 17850 69 42603405
Dyspnoea 52.74 15.59 65 17796 442556 42160918
Anogenital dysplasia 51.74 15.59 12 17849 130 42603344
Nephrolithiasis 51.35 15.59 70 17791 36760 42566714
Hemivertebra 51.33 15.59 12 17849 135 42603339
Pyelocaliectasis 51.05 15.59 20 17841 1389 42602085
Genital herpes 50.90 15.59 17 17844 745 42602729
Drug reaction with eosinophilia and systemic symptoms 49.86 15.59 74 17787 42001 42561473
HIV associated nephropathy 49.82 15.59 14 17847 340 42603134
Atrioventricular septal defect 48.89 15.59 13 17848 255 42603219
Nephropathy toxic 47.34 15.59 46 17815 16792 42586682
Hepatitis B 46.23 15.59 31 17830 6680 42596794
Genital herpes simplex 42.11 15.59 10 17851 121 42603353
Drug level increased 39.90 15.59 52 17809 26148 42577326
Adrenal insufficiency 37.66 15.59 43 17818 18881 42584593
Hepatocellular injury 37.63 15.59 48 17813 23630 42579844
Hepatitis C 36.90 15.59 32 17829 10101 42593373
Ectopic kidney 36.00 15.59 7 17854 29 42603445
Urinary tract inflammation 35.77 15.59 10 17851 238 42603236
Karyotype analysis abnormal 35.45 15.59 8 17853 76 42603398
Scrotal cyst 35.33 15.59 9 17852 148 42603326
Lipohypertrophy 33.79 15.59 10 17851 293 42603181
Superior mesenteric artery syndrome 33.59 15.59 8 17853 98 42603376
Rash maculo-papular 33.50 15.59 58 17803 37445 42566029
Low birth weight baby 33.38 15.59 30 17831 9925 42593549
Coarctation of the aorta 33.34 15.59 11 17850 464 42603010
Acute kidney injury 33.23 15.59 265 17596 367072 42236402
Congenital anomaly 32.83 15.59 15 17846 1526 42601948
Oesophageal atresia 32.17 15.59 11 17850 518 42602956
HIV lipodystrophy 32.11 15.59 6 17855 19 42603455
Peritoneal cyst 31.65 15.59 6 17855 21 42603453
Progressive multifocal leukoencephalopathy 31.46 15.59 31 17830 11505 42591969
Hepatic cancer 31.32 15.59 27 17834 8453 42595021
Congenital mitral valve incompetence 31.21 15.59 8 17853 135 42603339
Anal cancer stage 0 31.02 15.59 6 17855 24 42603450
Heart disease congenital 30.61 15.59 14 17847 1428 42602046
Anion gap abnormal 30.19 15.59 10 17851 427 42603047
Disease progression 28.91 15.59 12 17849 143644 42459830
Conductive deafness 28.54 15.59 10 17851 507 42602967
Congenital renal disorder 27.84 15.59 7 17854 109 42603365
CD4 lymphocytes abnormal 27.73 15.59 6 17855 46 42603428
Atrial fibrillation 27.55 15.59 12 17849 139581 42463893
Constipation 27.51 15.59 17 17844 162274 42441200
Blood pressure increased 27.03 15.59 5 17856 101923 42501551
Product residue present 26.77 15.59 16 17845 2825 42600649
Foetal death 26.57 15.59 8 17853 249 42603225
Acquired gene mutation 26.37 15.59 13 17848 1567 42601907
Foetal chromosome abnormality 26.27 15.59 5 17856 18 42603456
Drug level decreased 25.71 15.59 26 17835 9951 42593523
Hyperphagia 25.69 15.59 13 17848 1657 42601817
Cranial nerve palsies multiple 25.54 15.59 6 17855 69 42603405
Acute myocardial infarction 25.17 15.59 67 17794 58098 42545376
Glycosuria 25.06 15.59 12 17849 1358 42602116
Acquired immunodeficiency syndrome 24.91 15.59 9 17852 499 42602975
Maternal drugs affecting foetus 24.70 15.59 17 17844 3822 42599652
Neuropsychiatric symptoms 24.64 15.59 10 17851 762 42602712
Pneumonia 24.30 15.59 93 17768 422056 42181418
Cystitis noninfective 24.15 15.59 9 17852 545 42602929
HIV infection 24.14 15.59 12 17849 1473 42602001
Foetal growth restriction 24.07 15.59 19 17842 5264 42598210
Cushingoid 24.03 15.59 16 17845 3406 42600068
Immune reconstitution inflammatory syndrome associated tuberculosis 23.74 15.59 9 17852 572 42602902
Ergot poisoning 23.15 15.59 5 17856 38 42603436
Renal colic 23.08 15.59 13 17848 2055 42601419
Viral load abnormal 23.00 15.59 6 17855 109 42603365
Hyperlipidaemia 22.88 15.59 36 17825 21480 42581994
Peripheral swelling 22.74 15.59 5 17856 90265 42513209
Blood HIV RNA 22.72 15.59 4 17857 8 42603466
Pain 22.31 15.59 43 17818 244805 42358669
Leishmaniasis 22.24 15.59 8 17853 438 42603036
Pancreatitis 22.02 15.59 53 17808 43215 42560259
Anal cancer 21.92 15.59 8 17853 457 42603017
Cytomegalovirus chorioretinitis 21.91 15.59 17 17844 4594 42598880
Malignant neoplasm progression 21.89 15.59 9 17852 108391 42495083
Pulmonary sequestration 21.57 15.59 5 17856 54 42603420
Glucose tolerance impaired 21.34 15.59 16 17845 4108 42599366
Pneumocystis jirovecii pneumonia 21.26 15.59 38 17823 25143 42578331
Atrial septal defect 21.07 15.59 21 17840 7898 42595576
Inappropriate schedule of product administration 20.99 15.59 7 17854 95895 42507579
Blood triglycerides increased 20.33 15.59 29 17832 15867 42587607
Blood creatine phosphokinase increased 20.23 15.59 55 17806 48283 42555191
Liver function test abnormal 20.18 15.59 43 17818 32348 42571126
Relapsing fever 20.11 15.59 6 17855 181 42603293
Hyperphosphatasaemia 20.06 15.59 5 17856 75 42603399
Retinitis pigmentosa 19.95 15.59 4 17857 20 42603454
Small for dates baby 19.93 15.59 17 17844 5246 42598228
Hepatitis B DNA assay positive 19.88 15.59 5 17856 78 42603396
HIV wasting syndrome 19.82 15.59 5 17856 79 42603395
Product use complaint 19.57 15.59 12 17849 2219 42601255
Fanconi syndrome 19.27 15.59 11 17850 1783 42601691
Cortisol decreased 19.10 15.59 10 17851 1368 42602106
Congenital cerebral cyst 18.81 15.59 4 17857 28 42603446
Blood bilirubin increased 18.61 15.59 49 17812 42203 42561271
Renal tubular dysfunction 18.43 15.59 7 17854 447 42603027
Post transplant distal limb syndrome 18.38 15.59 7 17854 450 42603024
Anogenital warts 18.37 15.59 8 17853 727 42602747
Agranulocytosis 18.34 15.59 40 17821 30572 42572902
Mycobacterium avium complex immune restoration disease 18.34 15.59 4 17857 32 42603442
ECG signs of ventricular hypertrophy 18.26 15.59 3 17858 3 42603471
Oesophageal ulcer 18.17 15.59 14 17847 3745 42599729
Induration 18.13 15.59 9 17852 1101 42602373
Heart transplant rejection 18.09 15.59 10 17851 1524 42601950
Myelocytosis 18.02 15.59 4 17857 35 42603439
Amyotrophy 17.99 15.59 7 17854 477 42602997
Hyperproteinaemia 17.90 15.59 6 17855 266 42603208
Treatment failure 17.58 15.59 62 17799 62562 42540912
Hypercholesterolaemia 17.26 15.59 24 17837 12825 42590649
Congenital vesicoureteric reflux 17.19 15.59 4 17857 44 42603430
Coccidioidomycosis 17.14 15.59 8 17853 854 42602620
Chest discomfort 17.12 15.59 3 17858 63613 42539861
Skin test negative 17.11 15.59 4 17857 45 42603429
Retroperitoneal disorder 17.03 15.59 4 17857 46 42603428
Viraemia 16.76 15.59 10 17851 1760 42601714
Kaposi sarcoma inflammatory cytokine syndrome 16.69 15.59 5 17856 153 42603321
Joint swelling 16.67 15.59 4 17857 68018 42535456
Spinal compression fracture 16.60 15.59 18 17843 7465 42596009
Mitochondrial cytopathy 16.60 15.59 5 17856 156 42603318
Testicular mass 16.51 15.59 5 17856 159 42603315
Atypical mycobacterial infection 16.37 15.59 9 17852 1357 42602117
Meralgia paraesthetica 16.36 15.59 5 17856 164 42603310
Product use in unapproved therapeutic environment 16.28 15.59 6 17855 352 42603122
Vth nerve injury 16.18 15.59 3 17858 9 42603465
Hypo HDL cholesterolaemia 16.18 15.59 3 17858 9 42603465
Congenital ureteric anomaly 15.99 15.59 4 17857 61 42603413
Dermatitis exfoliative 15.92 15.59 17 17844 6930 42596544
Embolism 15.91 15.59 19 17842 8744 42594730
Pleocytosis 15.85 15.59 7 17854 658 42602816
Nephroangiosclerosis 15.63 15.59 5 17856 191 42603283

FDA Adverse Event Reporting System (Geriatric)

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
Drug interaction 770.83 16.94 684 20279 499499 110068837
Immune reconstitution inflammatory syndrome 719.34 16.94 219 20744 16007 110552329
Virologic failure 684.33 16.94 164 20799 4788 110563548
Abortion spontaneous 615.94 16.94 235 20728 34047 110534289
Lipodystrophy acquired 605.40 16.94 146 20817 4378 110563958
Exposure during pregnancy 474.25 16.94 329 20634 167095 110401241
Viral mutation identified 457.12 16.94 116 20847 4303 110564033
Mitochondrial toxicity 379.57 16.94 94 20869 3151 110565185
Progressive external ophthalmoplegia 375.98 16.94 80 20883 1340 110566996
Pathogen resistance 364.07 16.94 134 20829 17538 110550798
Blood HIV RNA increased 310.17 16.94 74 20889 2114 110566222
Eyelid ptosis 266.92 16.94 99 20864 13228 110555108
Treatment noncompliance 265.85 16.94 168 20795 72822 110495514
Viral load increased 263.81 16.94 71 20892 3319 110565017
Maternal exposure during pregnancy 232.05 16.94 263 20700 254620 110313716
Drug resistance 231.26 16.94 140 20823 56234 110512102
Genotype drug resistance test positive 201.61 16.94 48 20915 1358 110566978
Abortion induced 188.28 16.94 67 20896 7952 110560384
CD4 lymphocytes decreased 179.38 16.94 51 20912 2923 110565413
HIV-associated neurocognitive disorder 148.92 16.94 30 20933 378 110567958
Renal tubular disorder 148.05 16.94 55 20908 7374 110560962
Premature labour 147.24 16.94 58 20905 9114 110559222
Diplopia 141.48 16.94 92 20871 41802 110526534
Premature delivery 141.06 16.94 82 20881 30550 110537786
Foetal exposure during pregnancy 122.37 16.94 48 20915 7457 110560879
Adrenal suppression 120.18 16.94 33 20930 1663 110566673
CSF HIV escape syndrome 116.99 16.94 24 20939 333 110568003
Premature rupture of membranes 113.63 16.94 40 20923 4597 110563739
Syphilis 108.77 16.94 26 20937 748 110567588
Hepatocellular injury 107.94 16.94 84 20879 50558 110517778
Osteoporosis 105.89 16.94 105 20858 87047 110481289
Acute kidney injury 104.37 16.94 310 20653 635120 109933216
Osteonecrosis 101.60 16.94 69 20894 33672 110534664
Nephropathy toxic 99.34 16.94 63 20900 27415 110540921
Dyslipidaemia 98.97 16.94 52 20911 15913 110552423
Renal impairment 96.98 16.94 147 20816 188298 110380038
Hepatitis cholestatic 88.84 16.94 50 20913 17516 110550820
Stillbirth 82.88 16.94 31 20932 4233 110564103
Fanconi syndrome acquired 81.38 16.94 28 20935 3006 110565330
Cushingoid 80.81 16.94 41 20922 11671 110556665
Brain stem stroke 78.28 16.94 20 20943 761 110567575
Hypertriglyceridaemia 76.37 16.94 44 20919 16110 110552226
Rash maculo-papular 74.96 16.94 81 20882 74141 110494195
Ophthalmoplegia 73.37 16.94 27 20936 3523 110564813
Drug reaction with eosinophilia and systemic symptoms 73.30 16.94 84 20879 82011 110486325
Ectopic pregnancy 72.68 16.94 24 20939 2273 110566063
Live birth 68.72 16.94 75 20888 69409 110498927
Lipohypertrophy 68.63 16.94 19 20944 987 110567349
Pain 68.41 16.94 49 20914 954906 109613430
Joint swelling 67.92 16.94 4 20959 442841 110125495
Hepatitis C 64.15 16.94 36 20927 12537 110555799
Mycobacterium avium complex infection 63.41 16.94 28 20935 5849 110562487
Nephrolithiasis 61.22 16.94 69 20894 66143 110502193
Foetal death 61.03 16.94 38 20925 16007 110552329
HIV associated nephropathy 60.53 16.94 14 20949 348 110567988
Adrenal insufficiency 58.88 16.94 55 20908 42335 110526001
Infusion related reaction 56.79 16.94 4 20959 381158 110187178
Cholestasis of pregnancy 55.69 16.94 17 20946 1248 110567088
Genital herpes 54.97 16.94 20 20943 2527 110565809
Caesarean section 53.25 16.94 33 20930 13784 110554552
Hepatitis B DNA increased 53.08 16.94 15 20948 840 110567496
Premature baby 51.96 16.94 23 20940 4832 110563504
Alopecia 51.11 16.94 5 20958 364748 110203588
Psychomotor retardation 50.06 16.94 26 20937 7766 110560570
Dyspnoea 49.30 16.94 84 20879 1106788 109461548
Gene mutation 49.19 16.94 20 20943 3409 110564927
Nasopharyngitis 48.98 16.94 8 20955 394353 110173983
Gastroschisis 48.32 16.94 8 20955 29 110568307
Renal tubular dysfunction 48.03 16.94 14 20949 876 110567460
Anogenital dysplasia 47.07 16.94 10 20953 166 110568170
Fanconi syndrome 45.31 16.94 19 20944 3500 110564836
Multiple-drug resistance 44.50 16.94 29 20934 13206 110555130
Hyperadrenocorticism 43.96 16.94 12 20951 591 110567745
Urinary tract inflammation 43.88 16.94 11 20952 387 110567949
Complication of pregnancy 42.91 16.94 11 20952 424 110567912
Acute myocardial infarction 42.54 16.94 65 20898 83712 110484624
Anal cancer stage 0 41.74 16.94 7 20956 28 110568308
Arthralgia 41.69 16.94 52 20911 779580 109788756
Immune reconstitution inflammatory syndrome associated tuberculosis 41.48 16.94 13 20950 1041 110567295
Peripheral swelling 40.63 16.94 13 20950 404021 110164315
Renal colic 39.98 16.94 17 20946 3241 110565095
Hepatitis B 39.71 16.94 24 20939 9588 110558748
Liver function test abnormal 38.60 16.94 56 20907 68894 110499442
Abortion of ectopic pregnancy 37.97 16.94 7 20956 53 110568283
Endometritis decidual 37.91 16.94 6 20957 15 110568321
HIV lipodystrophy 37.91 16.94 6 20957 15 110568321
Progressive multifocal leukoencephalopathy 37.81 16.94 34 20929 24922 110543414
Sinusitis 36.87 16.94 6 20957 296682 110271654
Central obesity 36.67 16.94 14 20949 2022 110566314
Conductive deafness 36.40 16.94 9 20954 299 110568037
Genital herpes simplex 36.07 16.94 10 20953 522 110567814
Skin striae 35.61 16.94 14 20949 2187 110566149
Foetal growth abnormality 35.58 16.94 6 20957 25 110568311
Immunosuppressant drug level increased 35.34 16.94 24 20939 11700 110556636
Total bile acids increased 35.22 16.94 7 20956 82 110568254
Labelled drug-drug interaction medication error 35.00 16.94 35 20928 29267 110539069
Trisomy 21 34.76 16.94 7 20956 88 110568248
Wheezing 34.46 16.94 4 20959 255226 110313110
Abdominal discomfort 34.10 16.94 16 20947 393842 110174494
Hepatic cancer 34.02 16.94 23 20940 11133 110557203
Superior mesenteric artery syndrome 33.99 16.94 8 20955 215 110568121
Dermatitis exfoliative 33.66 16.94 23 20940 11324 110557012
Therapeutic product effect decreased 32.56 16.94 4 20959 244312 110324024
Proteinuria 32.46 16.94 39 20924 39979 110528357
Generalised anxiety disorder 32.45 16.94 14 20949 2765 110565571
Enzyme activity increased 32.04 16.94 5 20958 11 110568325
Gestational diabetes 31.95 16.94 19 20944 7370 110560966
Anion gap abnormal 31.61 16.94 10 20953 826 110567510
Mobility decreased 31.36 16.94 4 20959 237418 110330918
Infection 30.91 16.94 15 20948 362185 110206151
Amniotic cavity infection 30.81 16.94 10 20953 897 110567439
Swelling 30.79 16.94 14 20949 351027 110217309
Stomatitis 30.34 16.94 7 20956 270235 110298101
Cytomegalovirus chorioretinitis 29.97 16.94 18 20945 7110 110561226
Glycosuria 29.90 16.94 13 20950 2617 110565719
Blood HIV RNA 29.81 16.94 5 20958 20 110568316
Congenital intestinal malformation 29.62 16.94 5 20958 21 110568315
Eosinophilia 29.48 16.94 45 20918 57891 110510445
Fatigue 29.27 16.94 125 20838 1215833 109352503
Congenital multiplex arthrogryposis 29.25 16.94 5 20958 23 110568313
Pre-eclampsia 29.20 16.94 19 20944 8631 110559705
CD4 lymphocytes abnormal 28.87 16.94 6 20957 89 110568247
Pneumocystis jirovecii pneumonia 28.86 16.94 38 20925 42697 110525639
Renal tubular necrosis 28.57 16.94 32 20931 30443 110537893
Drug level increased 28.53 16.94 40 20923 47679 110520657
Cholestasis 28.53 16.94 47 20916 64471 110503865
Pulmonary sequestration 28.43 16.94 5 20958 28 110568308
Pericarditis 28.21 16.94 4 20959 219110 110349226
Oesophageal atresia 27.78 16.94 6 20957 108 110568228
Ventricular hypoplasia 27.51 16.94 4 20959 4 110568332
Discomfort 27.45 16.94 4 20959 214703 110353633
Neuropsychiatric symptoms 27.37 16.94 10 20953 1278 110567058
Diabetes mellitus 27.23 16.94 59 20904 99322 110469014
Glucocorticoids increased 27.09 16.94 6 20957 122 110568214
Polyhydramnios 26.79 16.94 11 20952 1922 110566414
Blood creatine phosphokinase increased 26.79 16.94 49 20914 73028 110495308
Wound 26.46 16.94 6 20957 234431 110333905
Musculoskeletal stiffness 26.40 16.94 10 20953 279812 110288524
Constipation 26.00 16.94 18 20945 357768 110210568
Pancytopenia 25.89 16.94 93 20870 209520 110358816
Vitamin D deficiency 25.62 16.94 24 20939 18528 110549808
Spina bifida 25.02 16.94 6 20957 175 110568161
Hypoplastic left heart syndrome 25.00 16.94 4 20959 11 110568325
Foetal growth restriction 24.98 16.94 12 20951 3038 110565298
Potassium wasting nephropathy 24.89 16.94 6 20957 179 110568157
Musculoskeletal pain 24.37 16.94 3 20960 183020 110385316
Coarctation of the aorta 24.33 16.94 5 20958 70 110568266
Oesophageal candidiasis 24.28 16.94 19 20944 11515 110556821
CSF test abnormal 24.16 16.94 8 20955 764 110567572
Pancreatitis acute 24.13 16.94 42 20921 60232 110508104
Blood triglycerides increased 23.95 16.94 26 20937 23900 110544436
Rhabdomyolysis 23.83 16.94 63 20900 120338 110447998
Abortion threatened 23.68 16.94 7 20956 460 110567876
HIV infection 23.61 16.94 9 20954 1294 110567042
Pain in extremity 23.46 16.94 35 20928 487083 110081253
Secondary adrenocortical insufficiency 23.45 16.94 13 20950 4421 110563915
Renal failure 23.43 16.94 95 20868 226479 110341857
Intentional product use issue 23.15 16.94 9 20954 247897 110320439
Teratogenicity 23.12 16.94 6 20957 243 110568093
White matter lesion 23.05 16.94 11 20952 2743 110565593
Prurigo 22.98 16.94 9 20954 1391 110566945
Face oedema 22.97 16.94 30 20933 33439 110534897
Cranial nerve palsies multiple 22.93 16.94 6 20957 251 110568085
Hepatic cytolysis 22.87 16.94 39 20924 55014 110513322
Cortisol decreased 22.74 16.94 11 20952 2825 110565511
Cushing's syndrome 22.70 16.94 8 20955 922 110567414
Dizziness 22.70 16.94 63 20900 698130 109870206
Atrioventricular septal defect 22.20 16.94 5 20958 110 110568226
Benign prostatic hyperplasia 22.18 16.94 22 20941 18212 110550124
Atrial fibrillation 22.01 16.94 8 20955 229634 110338702
Lactic acidosis 21.98 16.94 52 20911 92759 110475577
Testicular mass 21.78 16.94 5 20958 120 110568216
Pancreatitis 21.71 16.94 52 20911 93481 110474855
Hyperproteinaemia 21.63 16.94 6 20957 314 110568022
Product use in unapproved therapeutic environment 21.55 16.94 6 20957 318 110568018
Anogenital warts 21.14 16.94 8 20955 1128 110567208
Hyperphosphatasaemia 21.12 16.94 5 20958 138 110568198
Contusion 20.93 16.94 9 20954 233352 110334984
Lower respiratory tract infection 20.84 16.94 10 20953 243096 110325240
Drug intolerance 20.77 16.94 28 20935 406484 110161852
Retinopathy 20.76 16.94 12 20951 4417 110563919
ECG signs of ventricular hypertrophy 20.63 16.94 3 20960 3 110568333
Mitochondrial cytopathy 20.38 16.94 6 20957 389 110567947
Hyperbilirubinaemia 20.29 16.94 27 20936 30644 110537692
Retroperitoneal disorder 20.19 16.94 4 20959 46 110568290
Acquired gene mutation 20.05 16.94 10 20953 2744 110565592
New onset diabetes after transplantation 20 16.94 6 20957 415 110567921
Kaposi sarcoma inflammatory cytokine syndrome 20.00 16.94 5 20958 174 110568162
Encephalitis 19.78 16.94 21 20942 18818 110549518
Jaundice 19.57 16.94 38 20925 59198 110509138
Hydrocephalus 19.51 16.94 16 20947 10359 110557977
Relapsing fever 19.37 16.94 6 20957 462 110567874
Post transplant distal limb syndrome 19.30 16.94 7 20956 877 110567459
Blood pressure increased 18.76 16.94 13 20950 258360 110309976
Pneumonia 18.75 16.94 94 20869 876620 109691716
Memory impairment 18.64 16.94 7 20956 196937 110371399
Embolism 18.62 16.94 19 20944 16270 110552066
Hypo HDL cholesterolaemia 18.56 16.94 3 20960 9 110568327
Vth nerve injury 18.56 16.94 3 20960 9 110568327
Superinfection bacterial 18.32 16.94 9 20954 2392 110565944
Acute stress disorder 18.24 16.94 6 20957 561 110567775
Hepatitis acute 18.10 16.94 20 20943 18746 110549590
Inappropriate schedule of product administration 18.03 16.94 8 20955 203629 110364707
Eyelid oedema 17.80 16.94 18 20945 15244 110553092
Fall 17.77 16.94 57 20906 603425 109964911
Thrombocytopenia 17.70 16.94 120 20843 348765 110219571
Hypertrichosis 17.68 16.94 8 20955 1770 110566566
Back pain 17.52 16.94 27 20936 370969 110197367
Product use issue 17.46 16.94 20 20943 311675 110256661
Meningitis cryptococcal 17.41 16.94 11 20952 4751 110563585
Renal aneurysm 17.41 16.94 5 20958 297 110568039
Contraindicated product administered 17.36 16.94 13 20950 248254 110320082
Heart disease congenital 17.33 16.94 6 20957 656 110567680
Coagulation factor V level decreased 17.15 16.94 6 20957 677 110567659
Viral load abnormal 17.12 16.94 4 20959 104 110568232
Hyperlipidaemia 17.06 16.94 27 20936 35821 110532515
Amyotrophy 17.02 16.94 6 20957 692 110567644
Congestive cardiomyopathy 17.01 16.94 17 20946 14202 110554134

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AE10 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Protease inhibitors
ATC J05AR14 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR22 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR26 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
FDA MoA N0000000246 HIV Protease Inhibitors
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
MeSH PA D017320 HIV Protease Inhibitors
MeSH PA D019380 Anti-HIV Agents
FDA EPC N0000175889 Protease Inhibitor
FDA MoA N0000182137 Cytochrome P450 2D6 Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:35660 HIV protease inhibitor
CHEBI has role CHEBI:35718 antifungal agent
CHEBI has role CHEBI:36044 antiviral drug
CHEBI has role CHEBI:50864 insulin-sensitizing drug
CHEBI has role CHEBI:64946 anti-HIV agent

Related Drugs by ATC class:

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amprenaviratazanavirensitrelvirfosamprenavirindinavirnelfinavirnirmatrelvirritonavirsaquinavirtipranavir
J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
abacaviratazanavirbictegravircobicistatdolutegravirdoravirineefavirenzelvitegraviremtricitabinelamivudinelopinavirnevirapine show all 19 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus infection indication 86406008 DOID:526
Coronavirus infection off-label use 186747009
Hypercholesterolemia contraindication 13644009
Cirrhosis of liver contraindication 19943007 DOID:5082
Hereditary factor VIII deficiency disease contraindication 28293008 DOID:12134
Hereditary factor IX deficiency disease contraindication 41788008 DOID:12259
Hepatic failure contraindication 59927004
Chronic type B viral hepatitis contraindication 61977001
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Chronic hepatitis C contraindication 128302006
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Hypertriglyceridemia contraindication 302870006
Breastfeeding (mother) contraindication 413712001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.67 acidic
pKa2 1.64 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
150MG;EQ 675MG BASE PREZCOBIX JANSSEN PRODS N205395 March 21, 2025 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 25KG USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;EQ 800MG BASE PREZCOBIX JANSSEN PRODS N205395 Jan. 29, 2015 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 25KG USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;EQ 800MG BASE PREZCOBIX JANSSEN PRODS N205395 Jan. 29, 2015 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40KG USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;EQ 800MG BASE PREZCOBIX JANSSEN PRODS N205395 Jan. 29, 2015 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE IN ADULTS WHO ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE IN ADULTS WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PK ENHANCER THAT INHIBITS CY P450 MONOXYGENASE IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40KG WHO ARE VIROLOGICALLY SUPPRESSED ON A STABLE ARV REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TREATMENT OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PK ENHANCER THAT INHIBITS CY P450 MONOXYGENASE IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40KG WHO HAVE NO PRIOR ARV TREATMENT HISTORY
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TX OF HIV1 INFECTION USING A COMPOSITION CONTAINING A PK ENHANCER THAT INHIBITS CY P450 MONOXYGENASE IN ADULTS & PEDIATRIC PATIENTS AT LEAST 40KG HAVING NO PRIOR ARV TX HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ARV REGIMEN FOR AT LEAST 6 MO
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8148374 Sept. 3, 2029 TX OF HIV-1 INFECTION USING A COMPOSITION CONTAINING A PK ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENATES IN ADULTS WHO HAVE NO PRIOR ANTIRETROVIRAL TX HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV-1 INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40 KG WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV-1 INFECTION IN ADULTS WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV-1 INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 40 KG WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV-1 INFECTION IN ADULTS WHO HAVE NO PRIOR ANTIRETROVIRAL TREATMENT HISTORY OR ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN FOR AT LEAST 6 MONTHS
150MG;800MG;200MG;EQ 10MG BASE SYMTUZA JANSSEN PRODS N210455 July 17, 2018 RX TABLET ORAL 10786518 July 19, 2038 TREATMENT OF HIV-1 INFECTION IN ADULT OR PEDIATRIC PATIENTS (>=40 KG) WITH <50 COPIES/ML HIV-1 RNA AFTER >= 6 MONTHS ON PRIOR ANTIRETROVIRAL REGIMEN AND NO KNOWN DARUNAVIR OR TENOFOVIR RESISTANCE-ASSOCIATED SUBSTITUTIONS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Multidrug resistance protein 1 Transporter IC50 5.18 CHEMBL
Pol polyprotein Enzyme INHIBITOR Ki 10.85 CHEMBL CHEMBL
Gag-Pol polyprotein Polyprotein Ki 9.66 WOMBAT-PK
Protease Enzyme IC50 10.21 CHEMBL
Protease Enzyme Ki 10.96 CHEMBL
Protease Enzyme Ki 10.82 CHEMBL

External reference:

IDSource
4025441 VUID
N0000179778 NUI
D03656 KEGG_DRUG
635728-49-3 SECONDARY_CAS_RN
4025441 VANDF
4025493 VANDF
C1435444 UMLSCUI
CHEBI:367163 CHEBI
017 PDB_CHEM_ID
CHEMBL1323 ChEMBL_ID
CHEMBL1201127 ChEMBL_ID
D000069454 MESH_DESCRIPTOR_UI
DB01264 DRUGBANK_ID
11243 IUPHAR_LIGAND_ID
8305 INN_ID
YO603Y8113 UNII
213039 PUBCHEM_CID
460132 RXNORM
21619 MMSL
310017 MMSL
83005 MMSL
d05825 MMSL
011599 NDDF
011600 NDDF
423888002 SNOMEDCT_US
424096001 SNOMEDCT_US
428318002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 31722-088 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 31722-089 TABLET, FILM COATED 800 mg ORAL ANDA 27 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 31722-567 TABLET, FILM COATED 400 mg ORAL ANDA 27 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 31722-568 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 43598-704 TABLET, FILM COATED 600 mg ORAL ANDA 25 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 43598-705 TABLET, FILM COATED 800 mg ORAL ANDA 25 sections
PREZCOBIX HUMAN PRESCRIPTION DRUG LABEL 2 50090-1723 TABLET, FILM COATED 800 mg ORAL NDA 29 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 53808-0672 TABLET, FILM COATED 400 mg ORAL NDA 31 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 53808-0773 TABLET, FILM COATED 600 mg ORAL NDA 31 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 54868-5969 TABLET, FILM COATED 400 mg ORAL NDA 31 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 54868-6369 TABLET, FILM COATED 600 mg ORAL NDA 31 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 59676-562 TABLET, FILM COATED 600 mg ORAL NDA 31 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 59676-563 TABLET, FILM COATED 75 mg ORAL NDA 31 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 59676-564 TABLET, FILM COATED 150 mg ORAL NDA 31 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 59676-565 SUSPENSION 100 mg ORAL NDA 31 sections
PREZISTA HUMAN PRESCRIPTION DRUG LABEL 1 59676-566 TABLET, FILM COATED 800 mg ORAL NDA 31 sections
PREZCOBIX HUMAN PRESCRIPTION DRUG LABEL 2 59676-575 TABLET, FILM COATED 800 mg ORAL NDA 35 sections
PREZCOBIX PED HUMAN PRESCRIPTION DRUG LABEL 2 59676-577 TABLET, FOR SUSPENSION 600 mg ORAL NDA 35 sections
PREZCOBIX HUMAN PRESCRIPTION DRUG LABEL 2 59676-578 TABLET, FILM COATED 675 mg ORAL NDA 35 sections
Symtuza HUMAN PRESCRIPTION DRUG LABEL 4 59676-800 TABLET, FILM COATED 800 mg ORAL NDA 34 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 60219-1144 TABLET, FILM COATED 600 mg ORAL ANDA 27 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 60219-1145 TABLET, FILM COATED 800 mg ORAL ANDA 27 sections
DARUNAVIR HUMAN PRESCRIPTION DRUG LABEL 1 68180-345 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
DARUNAVIR HUMAN PRESCRIPTION DRUG LABEL 1 68180-345 TABLET, FILM COATED 600 mg ORAL ANDA 28 sections
DARUNAVIR HUMAN PRESCRIPTION DRUG LABEL 1 68180-346 TABLET, FILM COATED 800 mg ORAL ANDA 28 sections
DARUNAVIR HUMAN PRESCRIPTION DRUG LABEL 1 68180-346 TABLET, FILM COATED 800 mg ORAL ANDA 28 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 70771-1745 TABLET, FILM COATED 600 mg ORAL ANDA 1 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 70771-1746 TABLET, FILM COATED 800 mg ORAL ANDA 1 sections
Darunavir HUMAN PRESCRIPTION DRUG LABEL 1 71335-2611 TABLET, FILM COATED 800 mg ORAL ANDA 25 sections
Darunavir Human Prescription Drug Label 1 72205-184 TABLET, FILM COATED 600 mg ORAL ANDA 25 sections