# The Meandrous Route of Rilpivirine in the Search for the Miraculous Drug to Treat HIV Infections

**Authors:** Erik De Clercq

PMC · DOI: 10.3390/v17070959 · Viruses · 2025-07-08

## TL;DR

This paper discusses the development and use of rilpivirine, a drug for HIV treatment, combined with cabotegravir as a long-acting injection.

## Contribution

The paper highlights the clinical application and administration guidelines of long-acting CAB+RPV for HIV treatment.

## Key findings

- Rilpivirine combined with cabotegravir is used as a long-acting injection for HIV treatment.
- The combination is not recommended for patients with certain conditions like HBV infection or drug resistance.
- The treatment may cause injection site pain that diminishes over time.

## Abstract

Rilpivirine (RPV, R278474) was highlighted in 2005, two years after the death of Dr. Paul Janssen, as the ideal non-nucleoside reverse transcriptase inhibitor (NNRTI) to treat HIV infections. For this purpose, it was subsequently combined with tenofovir disoproxil fumarate (TDF), tenofovir alafenamide (TAF), darunavir (boosted with ritonavir or cobicistat) or dolutegravir. Its wide-spread use is thanks to its combination with cabotegravir (CAB) in the form of a long-acting intramuscular injection once per month (QM), later twice per month (Q2M), for the treatment of adults, later extended to adolescents and pregnant women, with HIV infections. The long-acting CAB plus RPV should not be administered in patients treated with rifampicin or rifabutin, patients with virological failure or patients with resistance to CAB or RPV, or patients with hepatitis B virus (HBV) infection. Long-acting CAB+RPV may lead to pain at the site of injection which would diminish over time.

## Linked entities

- **Chemicals:** rilpivirine (PubChem CID 6451164), tenofovir disoproxil fumarate (PubChem CID 5486830), tenofovir alafenamide (PubChem CID 461543), darunavir (PubChem CID 213039), ritonavir (PubChem CID 5076), cobicistat (PubChem CID 25151504), dolutegravir (PubChem CID 54726191), cabotegravir (PubChem CID 54713659), rifampicin (PubChem CID 135398735)

## Full-text entities

- **Diseases:** hepatitis B virus (HBV) infection (MESH:D006509), HIV Infections (MESH:D015658), pain (MESH:D010146)
- **Chemicals:** rifabutin (MESH:D017828), dolutegravir (MESH:C562325), TAF (MESH:C442442), cobicistat (MESH:D000069547), darunavir (MESH:D000069454), nucleoside (MESH:D009705), ritonavir (MESH:D019438), CAB (MESH:C584914), TDF (MESH:D000068698), R278474 (MESH:D000068696), rifampicin (MESH:D012293)
- **Species:** Homo sapiens (human, species) [taxon 9606]

## Full text

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## Figures

10 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12298302/full.md

## References

108 references — full list in the complete paper: https://tomesphere.com/paper/PMC12298302/full.md

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Source: https://tomesphere.com/paper/PMC12298302