rilpivirine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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: ONP

  • 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

Approvals:

DateAgencyCompanyOrphan
May 20, 2011 FDA JANSSEN PRODS
May 18, 2012 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
Viral load increased 327.32 39.25 52 1607 1322 63486041
Viral mutation identified 196.65 39.25 35 1624 1775 63485588
Virologic failure 189.08 39.25 34 1625 1828 63485535
Blood HIV RNA increased 147.20 39.25 24 1635 715 63486648
Exposure during pregnancy 140.43 39.25 72 1587 155475 63331888
Injection site nodule 118.83 39.25 26 1633 3809 63483554
Drug resistance 112.42 39.25 36 1623 22897 63464466
Pathogen resistance 85.67 39.25 22 1637 6376 63480987
Abortion spontaneous 80.33 39.25 34 1625 47161 63440202
Injection site pain 67.53 39.25 42 1617 129758 63357605
Product use in unapproved therapeutic environment 51.83 39.25 6 1653 9 63487354
Mycoplasma genitalium infection 49.01 39.25 6 1653 18 63487345

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 612.52 28.07 118 3291 2409 34951113
Virologic failure 256.57 28.07 61 3348 3419 34950103
Blood HIV RNA increased 158.29 28.07 34 3375 1196 34952326
Injection site pain 147.19 28.07 73 3336 38932 34914590
Viral mutation identified 128.67 28.07 34 3375 2920 34950602
Product use in unapproved therapeutic environment 121.71 28.07 17 3392 33 34953489
Pathogen resistance 100.62 28.07 37 3372 9445 34944077
Product dose omission issue 100.26 28.07 87 3322 119624 34833898
Product complaint 85.42 28.07 29 3380 5861 34947661
Injection site nodule 76.28 28.07 20 3389 1663 34951859
Pyelocaliectasis 58.85 28.07 15 3394 1115 34952407
Syphilis 50.17 28.07 11 3398 425 34953097
Wrong technique in device usage process 40.96 28.07 12 3397 1500 34952022
CD4 lymphocytes decreased 39.29 28.07 12 3397 1729 34951793
Blood triglycerides abnormal 37.98 28.07 8 3401 255 34953267
Drug resistance 34.89 28.07 25 3384 25902 34927620
Congenital hydronephrosis 34.60 28.07 9 3400 724 34952798
Glomerular filtration rate decreased 33.80 28.07 19 3390 12942 34940580
Foetal exposure during pregnancy 30.34 28.07 27 3382 38074 34915448
Blood HIV RNA below assay limit 30.17 28.07 4 3405 4 34953518

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 411.43 24.80 77 3631 2871 79737809
Viral mutation identified 215.19 24.80 47 3661 3811 79736869
Virologic failure 211.31 24.80 47 3661 4144 79736536
Blood HIV RNA increased 182.41 24.80 36 3672 1772 79738908
Drug resistance 130.66 24.80 55 3653 42158 79698522
Pathogen resistance 108.43 24.80 36 3672 14306 79726374
Product dose omission issue 95.18 24.80 84 3624 247453 79493227
Drug interaction 86.35 24.80 101 3607 415082 79325598
Product use in unapproved therapeutic environment 69.10 24.80 9 3699 24 79740656
Exposure during pregnancy 59.30 24.80 44 3664 101088 79639592
Product complaint 57.18 24.80 22 3686 13327 79727353
Injection site pain 55.72 24.80 47 3661 129791 79610889
Abortion spontaneous 51.94 24.80 26 3682 29481 79711199
Mycoplasma genitalium infection 45.55 24.80 6 3702 18 79740662
Injection site nodule 43.14 24.80 13 3695 3767 79736913
Blood triglycerides abnormal 38.87 24.80 8 3700 485 79740195
Syphilis 37.94 24.80 8 3700 546 79740134
Exposure via skin contact 35.90 24.80 7 3701 322 79740358
Gene mutation 33.97 24.80 10 3698 2676 79738004
Blood HIV RNA below assay limit 33.13 24.80 4 3704 4 79740676
Depressed mood 30.43 24.80 22 3686 48458 79692222
Hepatitis C 28.59 24.80 13 3695 11912 79728768
Melanoderma 28.53 24.80 6 3702 404 79740276
Facial paresis 26.88 24.80 10 3698 5516 79735164
Glomerular filtration rate decreased 25.89 24.80 15 3693 22687 79717993
Haemorrhoids thrombosed 25.28 24.80 5 3703 248 79740432
Ophthalmic herpes simplex 25.09 24.80 6 3702 724 79739956

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 D019380 Anti-HIV Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D044966 Anti-Retroviral Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D019384 Nucleic Acid Synthesis Inhibitors
MeSH PA D018894 Reverse Transcriptase Inhibitors
CHEBI has role CHEBI:50266 Prodrugs
CHEBI has role CHEBI:53756 reverse transcriptase inhibitors

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
200MG;EQ 25MG BASE;300MG COMPLERA GILEAD SCIENCES INC N202123 Aug. 10, 2011 RX TABLET ORAL 8592397 Jan. 13, 2024 TREATMENT OF HIV INFECTION
200MG;EQ 25MG BASE;300MG COMPLERA GILEAD SCIENCES INC N202123 Aug. 10, 2011 RX TABLET ORAL 8716264 Jan. 13, 2024 TREATMENT OF HIV INFECTION
200MG;EQ 25MG BASE;300MG COMPLERA GILEAD SCIENCES INC N202123 Aug. 10, 2011 RX TABLET ORAL 9457036 Jan. 13, 2024 TREATMENT OF HIV INFECTION
200MG;EQ 25MG BASE;300MG COMPLERA GILEAD SCIENCES INC N202123 Aug. 10, 2011 RX TABLET ORAL 9744181 Jan. 13, 2024 TREATMENT OF HIV INFECTION
EQ 25MG BASE EDURANT JANSSEN PRODS N202022 May 20, 2011 RX TABLET ORAL 7125879 April 21, 2025 IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV-1 INFECTION IN TREATMENT-NAIVE ADULT PATIENTS WITH HIV-1 RNA LESS THAN OR EQUAL TO 100,000 AT THE START OF THERAPY
EQ 25MG BASE EDURANT JANSSEN PRODS N202022 May 20, 2011 RX TABLET ORAL 7125879 April 21, 2025 IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV-1 INFECTION IN TREATMENT-NAIVE PATIENTS WITH HIV-1 RNA LESS THAN OR EQUAL TO 100,000 AT THE START OF THERAPY
EQ 25MG BASE EDURANT JANSSEN PRODS N202022 May 20, 2011 RX TABLET ORAL 7125879 April 21, 2025 IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS, IS INDICATED FOR THE TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN ANTIRETROVIRAL TREATMENT-NAIVE ADULT PATIENTS, AS SET FORTH IN THE LABELING, INCLUDING I&U SECTION
EQ 25MG BASE EDURANT JANSSEN PRODS N202022 May 20, 2011 RX TABLET ORAL 7125879 April 21, 2025 TREATMENT IN COMBINATION WITH CABOTEGRAVIR OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 AND OLDER TO REPLACE CURRENT REGIMEN IN THOSE WHO ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN WITH NO HISTORY OF TREATMENT FAILURE
200MG;EQ 25MG BASE;300MG COMPLERA GILEAD SCIENCES INC N202123 Aug. 10, 2011 RX TABLET ORAL 7125879 April 21, 2025 TREATMENT OF HIV INFECTION
200MG;EQ 25MG BASE;EQ 25MG BASE ODEFSEY GILEAD SCIENCES INC N208351 March 1, 2016 RX TABLET ORAL 7125879 April 21, 2025 TREATMENT OF HIV INFECTION
EQ 50MG BASE;EQ 25MG BASE JULUCA VIIV HLTHCARE N210192 Nov. 21, 2017 RX TABLET ORAL 7125879 April 21, 2025 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 7125879 April 21, 2025 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 7125879 April 21, 2025 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;300MG COMPLERA GILEAD SCIENCES INC N202123 Aug. 10, 2011 RX TABLET ORAL 8841310 Dec. 9, 2025 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 April 28, 2026 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 April 28, 2026 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 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 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 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
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

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. 31, 2025 NEW DOSING SCHEDULE FOR CABOTEGRAVIR/RILPIVRINE INJECTION EVERY 2 MONTHS
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR Jan. 31, 2025 NEW DOSING SCHEDULE FOR CABOTEGRAVIR/RILPIVRINE INJECTION EVERY 2 MONTHS
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR March 29, 2025 NEW PATIENT POPULATION
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR March 29, 2025 NEW PATIENT POPULATION
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

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 Unclassified 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
d07776 MMSL
013795 NDDF
013796 NDDF
703123005 SNOMEDCT_US
703124004 SNOMEDCT_US
703777002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Juluca HUMAN PRESCRIPTION DRUG LABEL 2 49702-242 TABLET, FILM COATED 25 mg ORAL NDA 28 sections
Juluca HUMAN PRESCRIPTION DRUG LABEL 2 49702-242 TABLET, FILM COATED 25 mg ORAL NDA 28 sections
Juluca HUMAN PRESCRIPTION DRUG LABEL 2 49702-242 TABLET, FILM COATED 25 mg ORAL NDA 28 sections
Juluca HUMAN PRESCRIPTION DRUG LABEL 2 49702-242 TABLET, FILM COATED 25 mg ORAL NDA 28 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 29 sections
EDURANT HUMAN PRESCRIPTION DRUG LABEL 1 59676-278 TABLET, FILM COATED 25 mg ORAL NDA 29 sections
EDURANT HUMAN PRESCRIPTION DRUG LABEL 1 59676-278 TABLET, FILM COATED 25 mg ORAL NDA 29 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
ODEFSEY HUMAN PRESCRIPTION DRUG LABEL 3 61958-2101 TABLET 25 mg ORAL NDA 35 sections
COMPLERA HUMAN PRESCRIPTION DRUG LABEL 3 70518-0677 TABLET, FILM COATED 25 mg ORAL NDA 30 sections