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

Stem definitionDrug idCAS RN
antivirals Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) 4174 500287-72-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rilpivirine
  • edurant
  • rilpivirine hydrochloride
  • rilpivirine HCl
A diarylpyrimidine derivative and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 that is used in the treatment of HIV INFECTIONS. It is also used in combination with other ANTI-HIV AGENTS, since ANTIVIRAL DRUG RESISTANCE emerges rapidly when it is used alone.
  • Molecular weight: 366.43
  • Formula: C22H18N6
  • CLOGP: 5.45
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 2
  • TPSA: 97.42
  • ALOGS: -4.50
  • ROTB: 5
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
25 mg O
15 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma) 0.00 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class AAK1,ABL1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,IKBKB,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK14,MAPK3,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK4,MELK,MET,MINK1,MST1R,MTOR,NTRK1,NTRK2,NUAK1,PAK1,PAK2,PAK4,PDGFRB,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKAA1,PRKAA2,PRKCD,PRKDC,PTK2,PTK6,RET,RIPK3,SGK1,SIK2,SIK3,SRC,STK10,STK11,STK33,STK4,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2,YES1,ZAP70 143
kinase-selectivity-class AAK1,ABL2,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK1,CDK2,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EPHA2,EPHB4,ERBB2,FLT3,GSK3A,GSK3B,IRAK1,IRAK3,JAK1,JAK2,LRRK2,MAP2K3,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MARK4,MET,NTRK1,PIK3CA,PIK3CG,PRKCD,RIPK3,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TGFBR1,TNIK,TTK,ULK1,ULK2 65
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
May 18, 2012 PMDA JANSSEN PHARMACEUTICAL K.K.
May 20, 2011 FDA JANSSEN PRODS

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
Viral load increased 611.28 35.23 95 3222 1461 90623669
Product use in unapproved therapeutic environment 389.41 35.23 47 3270 73 90625057
Virologic failure 376.81 35.23 66 3251 2158 90622972
Exposure during pregnancy 347.54 35.23 170 3147 238240 90386890
Viral mutation identified 295.84 35.23 53 3264 1972 90623158
Blood HIV RNA increased 284.19 35.23 45 3272 779 90624351
Pathogen resistance 232.92 35.23 55 3262 8060 90617070
Injection site nodule 202.58 35.23 44 3273 4429 90620701
Injection site pain 155.94 35.23 90 3227 173609 90451521
Product complaint 149.82 35.23 43 3274 13457 90611673
Product dose omission issue 142.45 35.23 103 3214 291584 90333546
Abortion spontaneous 137 35.23 57 3260 53999 90571131
Injection site discharge 129.01 35.23 25 3292 1426 90623704
Product storage error 116.54 35.23 39 3278 20202 90604928
Drug resistance 100.99 35.23 39 3278 30410 90594720
Injection site abscess 64.10 35.23 14 3303 1440 90623690
Wrong technique in device usage process 62.08 35.23 18 3299 5817 90619313
Occupational exposure to product 56.38 35.23 14 3303 2517 90622613
Mycoplasma genitalium infection 54.81 35.23 7 3310 21 90625109
Nodule 53.90 35.23 24 3293 26662 90598468
Incorrect dose administered 50.40 35.23 33 3284 78897 90546233
Hepatitis B reactivation 50.11 35.23 14 3303 3960 90621170
Atrioventricular septal defect 49.99 35.23 9 3308 342 90624788
Injection site mass 48.27 35.23 21 3296 22069 90603061
Treatment noncompliance 46.74 35.23 27 3290 51700 90573430
Injection site discomfort 40.42 35.23 13 3304 5927 90619203
Abortion induced 38.57 35.23 15 3302 11873 90613257
Congenital aortic valve incompetence 37.84 35.23 5 3312 21 90625109

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
Viral load increased 1355.39 28.89 259 7116 2738 42611222
Virologic failure 702.65 28.89 158 7217 3836 42610124
Product use in unapproved therapeutic environment 691.45 28.89 107 7268 251 42613709
Injection site pain 494.98 28.89 227 7148 57571 42556389
Blood HIV RNA increased 484.56 28.89 99 7276 1492 42612468
Pathogen resistance 472.25 28.89 143 7232 11307 42602653
Product dose omission issue 450.12 28.89 297 7078 154068 42459892
Viral mutation identified 391.15 28.89 95 7280 3236 42610724
Product storage error 317.41 28.89 105 7270 11035 42602925
Product complaint 269.33 28.89 80 7295 5897 42608063
Injection site nodule 200.24 28.89 51 7324 2110 42611850
Wrong technique in device usage process 128.93 28.89 38 7337 2719 42611241
Syphilis 113.00 28.89 25 7350 557 42613403
Injection site discomfort 112.61 28.89 33 7342 2313 42611647
Product administered at inappropriate site 91.34 28.89 30 7345 3068 42610892
Hepatitis B 75.35 28.89 32 7343 6679 42607281
Acute hepatitis B 66.97 28.89 14 7361 236 42613724
CD4 lymphocytes decreased 66.43 28.89 21 7354 1900 42612060
Inappropriate schedule of product administration 61.13 28.89 79 7296 95823 42518137
Hepatitis B reactivation 48.65 28.89 21 7354 4557 42609403
Substance use 47.79 28.89 16 7359 1735 42612225
Pyelocaliectasis 47.05 28.89 15 7360 1394 42612566
Treatment failure 46.95 28.89 56 7319 62568 42551392
Disseminated mycobacterium avium complex infection 44.60 28.89 10 7365 237 42613723
Myalgia 44.59 28.89 68 7307 96012 42517948
Injection site discharge 41.86 28.89 11 7364 514 42613446
Injection site mass 41.56 28.89 23 7352 8552 42605408
Lipodystrophy acquired 40.55 28.89 17 7358 3433 42610527
Viral load abnormal 40.00 28.89 8 7367 107 42613853
Pneumonia 39.63 28.89 12 7363 422137 42191823
Injection site reaction 37.73 28.89 27 7348 15694 42598266
Injection site induration 37.06 28.89 16 7359 3471 42610489
Pain 36.67 28.89 109 7266 244739 42369221
Viraemia 36.04 28.89 13 7362 1757 42612203
Depression 35.92 28.89 67 7308 111296 42502664
Injection site abscess 34.51 28.89 11 7364 1021 42612939
Blood triglycerides abnormal 33.34 28.89 8 7367 257 42613703
Single component of a two-component product administered 32.50 28.89 5 7370 11 42613949
Hepatitis C 30.46 28.89 20 7355 10113 42603847
Monkeypox 29.80 28.89 8 7367 406 42613554
Drug resistance 29.64 28.89 33 7342 34215 42579745
Beta 2 microglobulin urine increased 29.29 28.89 6 7369 91 42613869

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
Viral load increased 904.18 22.81 163 7556 3227 110578353
Virologic failure 577.40 22.81 119 7600 4833 110576747
Product use in unapproved therapeutic environment 541.51 22.81 76 7643 248 110581332
Viral mutation identified 519.90 22.81 107 7612 4312 110577268
Blood HIV RNA increased 504.01 22.81 93 7626 2095 110579485
Product dose omission issue 497.27 22.81 297 7422 321485 110260095
Pathogen resistance 487.18 22.81 132 7587 17540 110564040
Product storage error 437.86 22.81 127 7592 21601 110559979
Injection site pain 384.63 22.81 205 7514 177717 110403863
Product complaint 209.21 22.81 65 7654 13907 110567673
Injection site nodule 177.43 22.81 45 7674 4601 110576979
Injection site discomfort 141.76 22.81 41 7678 6866 110574714
Drug resistance 115.88 22.81 63 7656 56311 110525269
Wrong technique in device usage process 115.56 22.81 35 7684 6866 110574714
Hepatitis B reactivation 104.41 22.81 33 7686 7451 110574129
Syphilis 98.36 22.81 20 7699 754 110580826
Injection site discharge 96.38 22.81 22 7697 1438 110580142
Exposure during pregnancy 93.71 22.81 84 7635 167340 110414240
Abortion spontaneous 83.72 22.81 43 7676 34239 110547341
Hepatitis B 73.48 22.81 27 7692 9585 110571995
Inappropriate schedule of product administration 62.54 22.81 74 7645 203563 110378017
Blood triglycerides abnormal 61.89 22.81 13 7706 576 110581004
Drug interaction 58.63 22.81 116 7603 500067 110081513
Hepatitis C 56.32 22.81 24 7695 12549 110569031
Substance use 51.96 22.81 15 7704 2491 110579089
Treatment noncompliance 51.78 22.81 42 7677 72948 110508632
Mycoplasma genitalium infection 50.29 22.81 7 7712 21 110581559
CD4 lymphocytes decreased 45.18 22.81 14 7705 2960 110578620
Product administered at inappropriate site 44.39 22.81 16 7703 5377 110576203
Injection site abscess 41.56 22.81 12 7707 1994 110579586
Disseminated mycobacterium avium complex infection 40.70 22.81 9 7710 509 110581071
Acute hepatitis B 39.89 22.81 9 7710 558 110581022
Incorrect dose administered 37.43 22.81 41 7678 103600 110477980
Injection site induration 35.89 22.81 17 7702 11366 110570214
Lipodystrophy acquired 35.66 22.81 13 7706 4511 110577069
Gene mutation 35.23 22.81 12 7707 3417 110578163
Depressed mood 34.93 22.81 31 7688 60778 110520802
Nodule 34.83 22.81 24 7695 32607 110548973
Myalgia 34.09 22.81 58 7661 222323 110359257
Injection site mass 33.31 22.81 21 7698 24592 110556988
Monkeypox 32.19 22.81 7 7712 366 110581214
Product administration error 31.99 22.81 24 7695 37193 110544387
Beta 2 microglobulin urine increased 31.70 22.81 6 7713 155 110581425
Blood HIV RNA below assay limit 31.51 22.81 4 7715 4 110581576
Proctitis chlamydial 31.51 22.81 4 7715 4 110581576
Cryptosporidiosis infection 28.95 22.81 8 7711 1135 110580445
Injection site swelling 28.73 22.81 28 7691 61762 110519818
Abortion induced 28.46 22.81 13 7706 8006 110573574
Viral load abnormal 27.50 22.81 5 7714 103 110581477
HIV viraemia 26.81 22.81 5 7714 119 110581461
Viraemia 25.83 22.81 10 7709 4092 110577488
Erectile dysfunction 25.53 22.81 16 7703 18540 110563040
Injection site necrosis 25.51 22.81 8 7711 1758 110579822
Melanoderma 25.29 22.81 6 7713 464 110581116
Abdominal lymphadenopathy 25.24 22.81 8 7711 1820 110579760
Administration site discomfort 24.47 22.81 5 7714 193 110581387
Polycythaemia 24.29 22.81 9 7710 3266 110578314
Psychotic disorder 23.52 22.81 23 7696 50914 110530666
Chlamydial infection 23.34 22.81 6 7713 646 110580934
Depression 23.04 22.81 61 7658 317274 110264306

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AG05 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Non-nucleoside reverse transcriptase inhibitors
ATC J05AR08 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR19 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
ATC J05AR21 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HIV infections, combinations
FDA MoA N0000009948 Non-Nucleoside Reverse Transcriptase Inhibitors
FDA EXT N0000175460 Non-Nucleoside Analog
FDA EPC N0000175463 Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018894 Reverse Transcriptase Inhibitors
MeSH PA D019380 Anti-HIV Agents
MeSH PA D019384 Nucleic Acid Synthesis Inhibitors
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:53756 HIV-1 reverse transcriptase inhibitor
CHEBI has role CHEBI:59897 EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:50864 insulin-sensitizing drug

Related Drugs by ATC class:

J05AG Non-nucleoside reverse transcriptase inhibitors 5 drugs
delavirdinedoravirineefavirenzetravirinenevirapine
J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
abacaviratazanavirbictegravircobicistatdarunavirdolutegravirdoravirineefavirenzelvitegraviremtricitabinelamivudinelopinavir 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
Osteomalacia contraindication 4598005 DOID:10573
Hypophosphatemia contraindication 4996001
Suicidal thoughts contraindication 6471006
Torsades de pointes contraindication 31722008
Fanconi syndrome contraindication 40488004 DOID:1062
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Chronic type B viral hepatitis contraindication 61977001
Kidney disease contraindication 90708001 DOID:557
Lactic acidosis contraindication 91273001 DOID:3650
Prolonged QT interval contraindication 111975006
Liver function tests abnormal contraindication 166603001
Steatosis of liver contraindication 197321007
Disease of liver contraindication 235856003 DOID:409
Pathological fracture contraindication 268029009
Severe depression contraindication 310497006
Osteopenia contraindication 312894000
Breastfeeding (mother) contraindication 413712001
Obesity contraindication 414916001 DOID:9970
Congenital long QT syndrome contraindication 442917000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.48 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 11389447 June 30, 2027 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG BY MONTHLY ADMINISTRATION OF RILPIVIRINE SUSPENSION AS PART OF COMBINATION THERAPY
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 11389447 June 30, 2027 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG BY MONTHLY ADMINISTRATION OF RILPIVIRINE SUSPENSION AS PART OF COMBINATION THERAPY
EQ 50MG BASE;EQ 25MG BASE JULUCA VIIV HLTHCARE N210192 Nov. 21, 2017 RX TABLET ORAL 10426780 Jan. 24, 2031 TREATMENT OF HIV INFECTION
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 8410103 Feb. 4, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 8410103 Feb. 4, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 11224597 Sept. 15, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12138264 Sept. 15, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 11224597 Sept. 15, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12138264 Sept. 15, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR RE50189 Nov. 27, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR RE50189 Nov. 27, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
200MG;EQ 25MG BASE;EQ 25MG BASE ODEFSEY GILEAD SCIENCES INC N208351 March 1, 2016 RX TABLET ORAL 8754065 Aug. 15, 2032 TREATMENT OF HIV INFECTION
200MG;EQ 25MG BASE;EQ 25MG BASE ODEFSEY GILEAD SCIENCES INC N208351 March 1, 2016 RX TABLET ORAL 9296769 Aug. 15, 2032 TREATMENT OF HIV INFECTION
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12178815 July 18, 2038 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12178815 July 18, 2038 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12636285 Oct. 1, 2040 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12636286 Oct. 1, 2040 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12636285 Oct. 1, 2040 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12636286 Oct. 1, 2040 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR Jan. 21, 2026 NEW CHEMICAL ENTITY
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR Jan. 21, 2026 NEW CHEMICAL ENTITY
EQ 25MG BASE EDURANT JANSSEN PRODS N202022 May 20, 2011 RX TABLET ORAL March 15, 2027 NEW PATIENT POPULATION
EQ 2.5MG BASE EDURANT PED JANSSEN PRODS N219016 March 15, 2024 RX TABLET, FOR SUSPENSION ORAL March 15, 2027 NEW PRODUCT
EQ 25MG BASE EDURANT JANSSEN PRODS N202022 May 20, 2011 RX TABLET ORAL Sept. 15, 2027 PEDIATRIC EXCLUSIVITY
EQ 2.5MG BASE EDURANT PED JANSSEN PRODS N219016 March 15, 2024 RX TABLET, FOR SUSPENSION ORAL Sept. 15, 2027 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.30 CHEMBL
ATP-binding cassette sub-family G member 2 Transporter IC50 5.82 CHEMBL
Cytochrome P450 1A2 Enzyme IC50 5.04 CHEMBL
Reverse transcriptase/RNaseH Enzyme INHIBITOR IC50 9.17 CHEMBL CHEMBL
Reverse transcriptase Enzyme IC50 7.82 CHEMBL
Reverse transcriptase protein Enzyme EC50 9.10 CHEMBL

External reference:

IDSource
4030730 VUID
N0000182740 NUI
D09720 KEGG_DRUG
700361-47-3 SECONDARY_CAS_RN
4030730 VANDF
4030731 VANDF
C1566826 UMLSCUI
CHEBI:68606 CHEBI
T27 PDB_CHEM_ID
CHEMBL175691 ChEMBL_ID
CHEMBL1628504 ChEMBL_ID
D000068696 MESH_DESCRIPTOR_UI
DB08864 DRUGBANK_ID
11387 IUPHAR_LIGAND_ID
8469 INN_ID
FI96A8X663 UNII
6451164 PUBCHEM_CID
1102270 RXNORM
181475 MMSL
27887 MMSL
31577 MMSL
401419 MMSL
d07776 MMSL
013795 NDDF
013796 NDDF
703123005 SNOMEDCT_US
703124004 SNOMEDCT_US
703777002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Emtricitabine, Rilpivirine, Tenofovir Disoproxil Fumarate HUMAN PRESCRIPTION DRUG LABEL 3 0378-5440 TABLET, FILM COATED 25 mg ORAL ANDA 29 sections
emtricitabine, rilpivirine and tenofovir disoproxil fumarate Human Prescription Drug Label 3 42385-801 TABLET, FILM COATED 25 mg ORAL ANDA 28 sections
Rilpivirine Human Prescription Drug Label 1 42385-999 TABLET, FILM COATED 25 mg ORAL ANDA 27 sections
Juluca HUMAN PRESCRIPTION DRUG LABEL 2 49702-242 TABLET, FILM COATED 25 mg ORAL NDA 27 sections
Juluca HUMAN PRESCRIPTION DRUG LABEL 2 49702-242 TABLET, FILM COATED 25 mg ORAL NDA 27 sections
ODEFSEY HUMAN PRESCRIPTION DRUG LABEL 3 50090-2340 TABLET 25 mg ORAL NDA 30 sections
COMPLERA HUMAN PRESCRIPTION DRUG LABEL 3 54868-6360 TABLET, FILM COATED 25 mg ORAL NDA 32 sections
EDURANT HUMAN PRESCRIPTION DRUG LABEL 1 59676-278 TABLET, FILM COATED 25 mg ORAL NDA 34 sections
EDURANT PED HUMAN PRESCRIPTION DRUG LABEL 1 59676-280 TABLET, FOR SUSPENSION 2.50 mg ORAL NDA 34 sections
COMPLERA HUMAN PRESCRIPTION DRUG LABEL 3 61958-1101 TABLET, FILM COATED 25 mg ORAL NDA 31 sections
COMPLERA Access HUMAN PRESCRIPTION DRUG LABEL 3 61958-1102 TABLET, FILM COATED 25 mg ORAL EXPORT ONLY 33 sections
ODEFSEY HUMAN PRESCRIPTION DRUG LABEL 3 61958-2101 TABLET 25 mg ORAL NDA 35 sections
Rilpivirine HUMAN PRESCRIPTION DRUG LABEL 1 70069-848 TABLET, FILM COATED 25 mg ORAL ANDA 25 sections