Delving into the Latest Updates on Rilpivirine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

4-{[4-({4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile, Rilpivirine hydrochloride (JAN/USAN), RPV

+ [20]

Target

RT

Action

inhibitors

Mechanism

RT inhibitors(Viral reverse transcriptase inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication

HIV Infections

Inactive Indication

Acquired Immunodeficiency SyndromeContraceptionContraception Behavior+ [3]

Originator Organization

Janssen Global Services LLC

Active Organization

ViiV Healthcare Ltd.Janssen-Cilag International NVJanssen Products LP

+ [4]

Inactive Organization

Tibotec Pharmaceuticals

Janssen Sciences Ireland UC

Janssen Scientific Affairs LLC

+ [2]

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (20 May 2011),

HIV Infections

RegulationOrphan Drug (United States), Orphan Drug (Japan)

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Structure/Sequence

Molecular FormulaC22H19ClN6

InChIKeyKZVVGZKAVZUACK-BJILWQEISA-N

CAS Registry700361-47-3

People Living with HIV-1 (PLHIV) are an important group of patients attending their specialist's and continue growing thanks to efficacy antiretroviral treatment (ART), allowing them to stabilize the HIV-infection and to live a normal life despite the infection. The present study is encouraged to demonstrate that efficacy and security of CAB LA + RPV LA treatment's on this population remains the same compared to younger population of patients. This study also registers some metabolic and hepatic parameters to observe a hypothetical improvement on these parameters, as the population may suffer more comorbidities than younger population and therefore tolerability and convenience gains a huge importance on them. Psychosocial aspects are also very important in these patients as these patients may suffer social stigma, and therefore suffering certain psychological disorders.

Start Date03 Mar 2025

Sponsor / Collaborator

ViiV Healthcare Ltd.

TCTR20250218001

/ RecruitingPhase 3IIT

Changes in sleep quality following a switch of antiretroviral regimen from three to two drugs: A comparative study between dolutegravir and lamivudine (DTG + 3TC) and dolutegravir and rilpivirine (DTG + RPV)

Start Date04 Feb 2025

Sponsor / Collaborator-

100 Clinical Results associated with Rilpivirine Hydrochloride

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100 Translational Medicine associated with Rilpivirine Hydrochloride

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100 Patents (Medical) associated with Rilpivirine Hydrochloride

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1,988

Literatures (Medical) associated with Rilpivirine Hydrochloride

31 Dec 2025·JOURNAL OF MEDICAL ECONOMICS

Treatment persistence among treatment-experienced people with HIV switching to integrase strand transfer inhibitor–based antiretroviral regimens

Article

Author: Chen, Megan ; de Boer, Melanie ; Trom, Cassidy ; Chuo, Ching-Yi ; Christoph, Mary J. ; Zachry, Woodie

AIMS:

Low rates of persistence are associated with poor outcomes in people with HIV (PWH). This retrospective cohort study assessed treatment persistence as measured by time to treatment switch in treatment-experienced (TE) PWH initiating integrase strand transfer inhibitor (INSTI)-based regimens.

METHODS:

United States prescription claims and medical history data from the IQVIA Longitudinal Access and Adjudication Dataset between January 1, 2018, and August 31, 2023, were analyzed. TE PWH with ≥1 prescription claim for initiation of an INSTI-based antiretroviral regimen during the index period (January 1, 2020, to December 31, 2022) were included. Descriptive analyses of demographic and comorbidity variables were performed, stratified by regimen. Kaplan-Meier analysis was used to evaluate time to subsequent treatment switch in the overall population and among PWH aged ≥50 years, those receiving Medicare, and those with mental health conditions or substance use disorders.

RESULTS:

Overall, 29,348 TE PWH were included. The majority of INSTI-based regimen initiations were for bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF) (61%; n = 17,917), followed by dolutegravir/lamivudine (27.4%; n = 8034) and cabotegravir + rilpivirine (7.4%; n = 2186). A subsequent switch occurred in 3341 (11.4%) PWH. Risk factors for switch included female sex, Medicare/Medicaid coverage, and higher Charlson Comorbidity Index scores. B/F/TAF was associated with the fewest subsequent switches (9.2%; n = 1656) and was significantly less likely than any other regimen to lead to a subsequent switch, either in the overall population or in the three at-risk subgroups.

LIMITATIONS:

No data are available to determine the underlying reasons for initial treatment choice or subsequent treatment switch.

CONCLUSIONS:

This study provides evidence for greater treatment persistence with B/F/TAF versus other INSTI-based regimens. Unlike prior studies that focused on treatment-naïve individuals, this analysis uniquely evaluates persistence among treatment-experienced PWH initiating newer INSTI-based regimens.

01 Dec 2025·Current HIV/AIDS Reports

Long-Acting Injectable Antiretroviral Therapy for Treatment of Human Immunodeficiency Virus: A Review

Review

Author: Brotherton, Amy L ; Rossi, Michael R ; Beckwith, Curt G ; Sanchez, Martha C ; Johnson, Jennie E

PURPOSE OF REVIEW:

Long-acting injectable (LAI) antiretroviral therapy (ART) for treatment of HIV-1 are approved both as a complete treatment regimen (cabotegravir/rilpivirine) and as an additional treatment option (lenacapavir) for those with multidrug resistant HIV-1. Here, we review the data supporting these approvals, pharmacokinetics, and additional patient populations that many benefit from LAI ART.

RECENT FINDINGS:

Persons with HIV and adherence challenges as well as those in low-and-middle income countries have high rates of adherence and viral suppression with LAI ART. LAI cabotegravir/rilpivirine (CAB/RPV) offers an alternative treatment approach to daily oral ART for people with HIV-1 infection that is associated with high rates of patient satisfaction when compared to daily oral ART. LAI CAB/RPV is currently only approved in those with HIV-1 viral suppression, however recent data support the use of LAI ART in populations with adherence challenges. Furthermore, given high rates of NNRTI resistance globally, CAB/RPV is not recommended in low-and-middle income countries presently, although this recommendation is likely to change based on recently published data. More research is needed among groups that may benefit from long-acting treatments for HIV-1.

01 Nov 2025·BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and biological evaluation of N-acyl diaryl pyrimidines (NDAPYs) as novel reverse transcriptase inhibitors

Article

Author: Shaikh, Taslim B ; Alli, Vidya Jyothi ; Yadav, Pawan ; Grée, René ; Sule, Swapnil Anil ; Ahsan, Mohammed Jawed ; Jadav, Surender Singh ; Andugulapati, Sai Balaji

Diaryl pyrimidines (DAPYs) are privileged structures for Non-Nucleosidic Reverse Transcriptase Inhibitors (NNRTIs), and they are considered as one of the fundamental scaffolds of existing anti-HIV agents. In this study, we designed novel molecules by the addition of a N-acyl group to the C4-position of Rilpivirine/Etravirine basic scaffold, a well-known class of DAPYs, in order to provide more interactions with K103 and E138 in Reverse Transcriptase. This was leading, as expected, to better in vitro RT inhibition, and the compounds 12c (56 %) and 12 k (49 %) demonstrated three-fold higher potency than Doravirine (17 %). Additionally, compound 12c was identified as a strong and 12k as a moderate HIV reverse transcriptase enzyme inhibitor in the in vitro experiments. DAPYs are also crucial in the development of novel anti-cancer agents targeting several kinases, and our compounds, 12d and 12j, exhibited moderate cytotoxicity with IC₅₀ values of 14.21 and 10.16 μM, respectively, against PC-3 cells and caused cell cycle arrest at G2/M checkpoint. The compound 12d induced apoptosis and reduced angiogenesis in PC-3 cells. Additionally, preliminary kinase screening against a panel of eight human kinases demonstrated only low PIM1 inhibition. However, the absence of correlation with cytotoxicity advocates an alternative mode of action that ought to be determined. Altogether, these studies indicate that the C4-position of diaryl pyrimidines could be important and warrants further investigated towards optimization of potential reverse transcriptase inhibitors.

126

News (Medical) associated with Rilpivirine Hydrochloride

24 Jul 2025

·www.shionogi.com

ViiV Healthcare’s Presentation on the VOLITION Study of Long-Acting Injectable Cabenuva in HIV Treatment

• 89% of people living with HIV expressed a preference to switch from daily oral therapy to long-acting injectable Cabenuva OSAKA, Japan, July 24, 2025 - Shionogi & Co., Ltd. (Head Office: Osaka, Japan; Chief Executive Officer: Isao Teshirogi, Ph.D.; hereafter "Shionogi") announced that ViiV Healthcare Ltd. (“ViiV”), in which Shionogi holds equity alongside GlaxoSmithKline plc and Pfizer Inc., has presented results from the Phase IIIb VOLITION study of Cabenuva at the 13th International AIDS Society Conference (IAS 2025). The VOLITION study was conducted in treatment-naïve adults living with HIV. Following rapid viral suppression with daily oral Dovato (dolutegravir and lamivudine), participants were offered the choice to either continue with Dovato or switch to the long-acting injectable Cabenuva (cabotegravir and rilpivirine). Results showed that 89% (n=129/145) of participants chose to switch to Cabenuva. The most commonly cited reasons were “Not having to worry about missing a dose each day” (80%) and “Not having to carry medication” (68%). These findings highlight the potential of long-acting regimens to improve adherence and overall treatment satisfaction among people living with HIV. Shionogi has positioned “Protect people from the threat of infectious diseases” as one of its key material issues and is committed to addressing the three major infectious diseases—HIV, tuberculosis, and malaria—through comprehensive initiatives. With over 60 years of experience in infectious disease research and development, Shionogi will continue to work in partnership with ViiV Healthcare to contribute to global health by advancing both treatment and prevention strategies for HIV. Reference: About Dovato (marketed in Japan as Dovato Combination Tablets) Dovato is a daily oral two-drug regimens containing dolutegravir 50 mg and lamivudine 300 mg. It is approved for the treatment of HIV-1 infection in adults who are either treatment-naïve or virologically suppressed on antiretroviral therapy, with no known resistance to dolutegravir or lamivudine. About Cabenuva (marketed in Japan as Vocabria Intramuscular Suspension and Rekambys® Intramuscular Suspension) Cabenuva is the world’s first long-acting injectable for HIV treatment. It is approved in major markets including Japan, the U.S., Europe, and China as a treatment option administered once every two months.1 In addition to the results of this study, multiple real-world data led by ViiV Healthcare—including COMBINE-2, CARLOS, BEYOND, and OPERA—have demonstrated high efficacy, tolerability, and improved adherence, contributing to enhanced treatment satisfaction across a broad range of patient populations.2 1. ViiV Healthcare Press Release: February 26, 2024 LATITUDE PHASE III INTERIM TRIAL DATA INDICATES ViiV HEALTHCARE’S LONG-ACTING INJECTABLE HIV TREATMENT CABENUVA (CABOTEGRAVIR + RILPIVIRINE) HAS SUPERIOR EFFICACY COMPARED TO DAILY THERAPY IN INDIVIDUALS LIVING WITH HIV WHO HAVE ADHERENCE CHALLENGES 2. ViiV Healthcare Press Release: July 14, 2025 ViiV HEALTHCARE DATA SHOW 89% OF TREATMENT-NAÏVE PEOPLE WITH HIV CHOOSE TO SWITCH TO LONG-ACTING INJECTABLE VOCABRIA + REKAMBYS FROM DAILY PILLS AFTER ACHIEVING RAPID VIRAL SUPPRESSION Forward-Looking Statements This announcement contains forward-looking statements. These statements are based on expectations in light of the information currently available, assumptions that are subject to risks and uncertainties which could cause actual results to differ materially from these statements. Risks and uncertainties include general domestic and international economic conditions such as general industry and market conditions, and changes of interest rate and currency exchange rate. These risks and uncertainties particularly apply with respect to product-related forward-looking statements. Product risks and uncertainties include, but are not limited to, completion and discontinuation of clinical trials; obtaining regulatory approvals; claims and concerns about product safety and efficacy; technological advances; adverse outcome of important litigation; domestic and foreign healthcare reforms and changes of laws and regulations. Also for existing products, there are manufacturing and marketing risks, which include, but are not limited to, inability to build production capacity to meet demand, lack of availability of raw materials and entry of competitive products. The company disclaims any intention or obligation to update or revise any forward-looking statements whether as a result of new information, future events or otherwise. For Further Information, Contact: SHIONOGI Website Inquiry Form: https://www.shionogi.com/global/en/contact.html

Phase 3Clinical ResultDrug Approval

15 Jul 2025

·www.fiercepharma.com

GSK expands Medicines Patent Pool deal to allow generic production of cabotegravir for HIV treatment

Through the Medicines Patent Pool, GSK will allow generic drugmakers to produce and supply their versions of long-acting injectable cabotegravir as part of a treatment to HIV patients in poorer nations. GSK has expanded its voluntary licensing agreement with the United Nations-backed Medicines Patent Pool (MPP) for cabotegravir, allowing it to be produced by three generic drugmakers and supplied to patients in poorer nations for HIV treatment.The adjustment comes the same day that the World Health Organization (WHO) updated its guidance, recommending the long-acting injectable combo treatment of Cabenuva, or cabotegravir and rilpivirine, as an alternative to daily oral therapy for patients who are virally suppressed.Rilpivirine, which was developed by Johnson & Johnson and is known commercially in its oral formulation as Edurant, was approved by the FDA as an HIV treatment in 2011 and already has generic versions available outside the U.S.“This step is closely aligned with WHO’s new recommendation of long-acting injectable antiretrovirals as an alternative for people who are virologically suppressed but face adherence challenges with daily oral regimens,” Meg Doherty, the director of the WHO’s global HIV, hepatitis and STI programs, said in a release.The agreement comes on top of a licensing deal in 2022, which allowed specified generic drugmakers to produce their versions of cabotegravir for pre-exposure prophylaxis (PrEP). The long-acting drug, injected every two months, earned an FDA approval in 2021 under the brand name Apretude as a single agent for HIV prevention. The MPP licensing deal allows generic drugmakers Aurobindo, Cipla and Viatris to produce and supply their version of the treatment to all countries in Sub-Saharan Africa, as well as those in the world classified as low-income and lower-middle-income. The deal covers 133 nations.“Expanding access to long-acting options like this supports a more person-centered, choice- and needs-driven approach, which is exactly what an equitable and effective HIV response requires,” Charles Gore, the executive director of the MPP, added in a release. The agreement comes a week after Gilead signed on to provide its newly approved long-acting, injected PrEP drug Yeztugo at a not-for-profit rate to poorer nations around the world. The deal was struck with the Global Fund to Fight AIDS, Tuberculosis and Malaria and is designed to provide coverage for up to 2 million people over three years. Before that, Gilead had inked agreements with six generic drug manufacturers to make and sell Yeztugo across 120 high-incidence, resource-limited countries.Last month, the FDA signed off on Yeztugo as a twice-yearly alternative to Apretude.

License out/inDrug Approval

15 Jul 2025

·pharma.economictimes.indiatimes.com

Aurobindo to produce, supply long acting HIV treatment drug

New Delhi: Aurobindo Pharma on Tuesday said it will manufacture and supply the long-acting injectable HIV treatment cabotegravir across 133 countries. The Hyderabad-based drugmaker has been selected as one of the generic manufacturers under the expanded voluntary licensing agreement between the Medicines Patent Pool (MPP) and ViiV Healthcare, the company said in a statement. The agreement allows Aurobindo to manufacture and supply the long-acting injectable HIV treatment across 133 countries, including several low and middle-income markets, it added. This update now includes long-acting cabotegravir (CAB LA) for HIV treatment, in addition to its earlier use for prevention only. The treatment offers an alternative to daily pills, allowing patients to receive just one injection every one or two months. "We are privileged to be part of the sub-license expansion from MPP and ViiV to develop, manufacture, and distribute generic CAB LA in select markets for the treatment of HIV-1, in addition to the voluntary licence for PrEP," Aurobindo Pharma Vice Chairman & Managing Director K Nithyananda Reddy said. This is a significant and timely step towards increasing access to advanced long-acting treatment in LMICs, he added. Aurobindo remains committed to leveraging its global supply capabilities to make this vital combination long-acting injection therapy widely available and affordable, he stated. The consideration by ViiV and MPP to include the private market in royalty-bearing countries is a critical step toward expanding access across both public and private sectors, it added. ViiV Healthcare, the global specialist HIV company majority owned by GSK, with Pfizer and Shionogi as shareholders, and the Medicines Patent Pool (MPP), have announced an update to their voluntary licensing agreement to include patents relating to its use in a long-acting regimen. The announcement follows updated guidance from the WHO recommending long-acting injectable cabotegravir + rilpivirine as an HIV treatment option. Existing generic licensees for prevention will be able to develop, manufacture and supply generic CAB LA, for use in combination with long-acting rilpivirine, subject to required regulatory approvals, to help enable access to the long-acting treatment in 133 countries worldwide. This includes all least-developed, low-income, lower middle-income, and Sub-Saharan African countries, as well as countries where ViiV does not have patent rights for cabotegravir.

License out/in

100 Deals associated with Rilpivirine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D09720 D09958	Rilpivirine Hydrochloride	J05AG05	DB08864

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
HIV Infections	United States	Janssen Products LP	20 May 2011

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pregnancy	Phase 3	United States	Janssen Scientific Affairs LLC	09 Apr 2009
Pregnancy	Phase 3	Puerto Rico	Janssen Scientific Affairs LLC	09 Apr 2009
Hepatitis	Phase 1	United States	ViiV Healthcare Ltd.	01 Nov 2011
Hepatitis C	Phase 1	-	Tibotec Pharmaceuticals	01 Nov 2010
Contraception	Phase 1	-	Tibotec Pharmaceuticals	01 Jul 2008
Contraception Behavior	Phase 1	-	Tibotec Pharmaceuticals	01 Jul 2008
Acquired Immunodeficiency Syndrome	Phase 1	-	Tibotec Pharmaceuticals	01 Jun 2008

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03635788 (LATITUDE , CTgov)	Phase 3	HIV Infections	456	CAB-LA Maintenance Dose+Oral CAB+RPV-LA Loading Dose (Step 2 Arm A: LA ART)	ortgxvfwmp = byhdtgyofw juoaxguhov (jxqxlflozv, zkyudnmvkn - jsmbzowlsk) View more	-	24 Apr 2025
				Standard of Care (SOC) Oral ART (Step 2 Arm B: SOC)	ortgxvfwmp = cexcodvfoh juoaxguhov (jxqxlflozv, yjmkbxcsqc - iohsqgpuor) View more
NCT03497676 (IMPAACT 2017/MOCHA, Pubmed \| Lancet HIV)	Phase 1/2	HIV Infections	139	Long-acting Injectable Cabotegravir 600 mg + Long-acting Injectable Rilpivirine 900 mg	vdzpfwzyyu(kljryifihx) = 10.8% [95% CI 6.2-17.2] of all 139 participants in the evaluable analysis population had at least one adverse event of grade 3 or above by week 24 rzkspkmqby (mmmjghedzc ) View more	Positive	01 Mar 2025
NCT00799864 (PAINT, CTgov)	Phase 2	HIV Infections	54	Rilpivirine (Cohort 1 Adolescents: Rilpivirine 25 mg)	tphqxqddjc(vziacjqfjg) = fvnpuazgtv axnnjkmbns (zzaegwfsuf, 38.0) View more	-	25 Jun 2024
				Rilpivirine (Cohort 2 Children (>=25 kg): Rilpivirine 25 mg)	tphqxqddjc(vziacjqfjg) = mcykaiafox axnnjkmbns (zzaegwfsuf, 52.2) View more
NCT04012931 (CTgov)	Phase 2	HIV Infections	26	Rilpivirine (Rilpivirine 12.5 Milligrams (mg) (<20 kg))	qmbyvudlhh(lmzbkfuvrc) = jhpobsnaty rkadfpmews (xudkvegplu, NA) View more	-	02 May 2024
				Rilpivirine (Rilpivirine 15 mg (<20 kg))	ghkdbifydv(cuudzqdndb) = ulpgrezoka yrlygpsusq (wvuowsgnkz, NA) View more
TMC278-C213 (FDA) Manual	Phase 2	HIV Infections	-	EDURANT+BR (HIV RNA ≤100,000)	rgwbowxfuf(atpbarigqn) = zfidonqxss bjcvzafwmm (tsaazifyqd ) View more	Superior	15 Mar 2024
				EDURANT+BR (HIV RNA >100,000)	rgwbowxfuf(atpbarigqn) = amzuswoyco bjcvzafwmm (tsaazifyqd ) View more
NCT00543725 \| NCT00540449 (THRIVE, FDA) Manual	Phase 3	HIV Infections	-	EDURANT + BR	tptkynmwdo(ohmjkandqk) = lwybwpxvzx efzqjqffno (xztywrkylq ) View more	Superior	15 Mar 2024
				Efavirenz + BR	tptkynmwdo(ohmjkandqk) = oefeyajltp efzqjqffno (xztywrkylq ) View more
NCT04399551 (CARISEL, CTgov)	Phase 3	HIV Infections	437	Continuous Quality Improvement (CQI) calls	ynbzoofisv = dvwjaszmuo kcjatbgcsb (gcsktvcyyu, zqbsekwtgj - gejethhzau)	-	19 May 2023
NCT04399551 (CARISEL, Corporate Publications) Manual	Phase 3	HIV Infections	437	Cabotegravir+Rilpivirine Hydrochloride	hvxqgevldj(grynvknvom) = kalhflytzt azzixjvzgq (csbpjkzxmz ) View more	Positive	24 Oct 2022
NCT03639311 (Pubmed) Manual	Phase 2	HIV Infections	97	CAB+RPV long-acting	mejulfuupk(lwccsgnuek) = hlcpzgpyer mapkfvhhbv (puvigschmy ) View more	Positive	01 Feb 2022
				dolutegravir/RPV	mejulfuupk(lwccsgnuek) = erebxacpby mapkfvhhbv (puvigschmy ) View more
NCT04001803 (CUSTOMIZE, CTgov)	Phase 3	HIV Infections	115	CAB+RPV LA (Staff Study Participants)	aydioecxfx(feymtqfjxr) = tglpmbjnqw spxadcmjox (dhfrorehny, 0.42) View more	-	10 Jan 2022
				long-acting (LA)+CAB LA+Rilpivirine (RPV) (Participants With HIV Infection)	jwahzkhlis(ntdjmyaypl) = xnyghfwler ffgouqeetu (qbcrygdvek, 0.74) View more