rilpivirine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) | 4174 | 500287-72-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 25 | mg | O |
| 15 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 20, 2011 | FDA | JANSSEN PRODS | |
| May 18, 2012 | PMDA | JANSSEN PHARMACEUTICAL K.K. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.48 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |