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

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
Drug resistance 118.63 39.87 33 881 18956 50585254
Viral mutation identified 110.68 39.87 20 894 1609 50602601
Virologic failure 98.43 39.87 18 896 1546 50602664
Exposure during pregnancy 85.21 39.87 42 872 120973 50483237
Abortion spontaneous 63.60 39.87 25 889 41747 50562463
Blood HIV RNA increased 52.35 39.87 9 905 540 50603670
Viral load increased 51.73 39.87 10 904 1153 50603057
Mycoplasma genitalium infection 51.23 39.87 6 908 18 50604192

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
Virologic failure 135.97 27.68 32 1739 2815 29569941
Viral mutation identified 83.19 27.68 21 1750 2467 29570289
Blood HIV RNA increased 67.62 27.68 15 1756 1009 29571747
Pyelocaliectasis 66.43 27.68 15 1756 1094 29571662
Pathogen resistance 51.24 27.68 19 1752 8097 29564659
Viral load increased 47.79 27.68 13 1758 2036 29570720
Drug interaction 46.69 27.68 58 1713 197327 29375429
Foetal exposure during pregnancy 45.10 27.68 27 1744 33840 29538916
Syphilis 39.69 27.68 8 1763 338 29572418
Congenital hydronephrosis 39.35 27.68 9 1762 694 29572062
Glomerular filtration rate decreased 38.61 27.68 17 1754 11249 29561507
Drug resistance 33.49 27.68 19 1752 21521 29551235
Facial paresis 31.65 27.68 10 1761 2631 29570125
Ophthalmic herpes simplex 29.61 27.68 6 1765 260 29572496
Pancreatic failure 28.77 27.68 7 1764 704 29572052

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 mutation identified 131.47 29.43 29 2204 3317 64493182
Virologic failure 124.97 29.43 28 2205 3438 64493061
Drug resistance 122.82 29.43 46 2187 35056 64461443
Drug interaction 97.32 29.43 88 2145 361995 64134504
Blood HIV RNA increased 59.03 29.43 13 2220 1471 64495028
Exposure during pregnancy 52.64 29.43 33 2200 77642 64418857
Abortion spontaneous 50.03 29.43 22 2211 25121 64471378
Mycoplasma genitalium infection 47.32 29.43 6 2227 18 64496481
Gene mutation 39.42 29.43 10 2223 2072 64494427
Syphilis 35.36 29.43 7 2226 471 64496028
Depressed mood 31.77 29.43 19 2214 40993 64455506
Pathogen resistance 31.66 29.43 13 2220 12530 64483969
Melanoderma 31.02 29.43 6 2227 358 64496141
Facial paresis 30.97 29.43 10 2223 4882 64491617

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 (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;EQ 25MG BASE ODEFSEY GILEAD SCIENCES INC N208351 March 1, 2016 RX TABLET ORAL 7803788 Feb. 2, 2022 TREATMENT OF HIV INFECTION
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 THEARPY
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
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
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
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
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
COMPLERA HUMAN PRESCRIPTION DRUG LABEL 3 70518-0677 TABLET, FILM COATED 25 mg ORAL NDA 30 sections