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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
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

Molecule

Description

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:

Dose	Unit	Route
25	mg	O
15	mg	P

ADMET properties:

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Property	Value	Reference
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

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Approvals:

Date	Agency	Company	Orphan
May 18, 2012	PMDA	JANSSEN PHARMACEUTICAL K.K.
May 20, 2011	FDA	JANSSEN PRODS

FDA Adverse Event Reporting System (Female)

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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 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

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FDA Adverse Event Reporting System (Male)

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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 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

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FDA Adverse Event Reporting System (Geriatric)

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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 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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:53756	reverse transcriptase inhibitors
FDA EPC	N0000175463	Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor
FDA EXT	N0000175460	Non-Nucleoside Analog
FDA MoA	N0000009948	Non-Nucleoside Reverse Transcriptase Inhibitors
MeSH PA	D019380	Anti-HIV Agents

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

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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

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🐶 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)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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
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;300MG	COMPLERA	GILEAD SCIENCES INC	N202123	Aug. 10, 2011	RX	TABLET	ORAL	8841310	Dec. 9, 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
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	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

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Orange Book exclusivity data (new drug applications)

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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
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
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. 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	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	Jan. 21, 2026	NEW CHEMICAL ENTITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.30	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.82	CHEMBL
Cytochrome P450 1A2	Enzyme	P05177	CP1A2_HUMAN		IC50	5.04	CHEMBL
Reverse transcriptase/RNaseH	Enzyme		Q72547_9HIV1	INHIBITOR	IC50	9.17	CHEMBL	CHEMBL
Reverse transcriptase	Enzyme		Q9WKE8_9HIV1		IC50	7.82	CHEMBL
Reverse transcriptase protein	Unclassified		Q9WJQ2_9HIV1		EC50	9.10	CHEMBL

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External reference:

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ID	Source
T27	PDB_CHEM_ID
013795	NDDF
013796	NDDF
1102270	RXNORM
11387	IUPHAR_LIGAND_ID
181475	MMSL
27887	MMSL
31577	MMSL
4030730	VUID
4030730	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
COMPLERA	HUMAN PRESCRIPTION DRUG LABEL	3	54868-6360	TABLET, FILM COATED	25 mg	ORAL	NDA	32 sections
COMPLERA	HUMAN PRESCRIPTION DRUG LABEL	3	61958-1101	TABLET, FILM COATED	25 mg	ORAL	NDA	31 sections
COMPLERA	HUMAN PRESCRIPTION DRUG LABEL	3	70518-0677	TABLET, FILM COATED	25 mg	ORAL	NDA	30 sections
COMPLERA Access	HUMAN PRESCRIPTION DRUG LABEL	3	61958-1102	TABLET, FILM COATED	25 mg	ORAL	EXPORT ONLY	33 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
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

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