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The acyclic nucleoside phosphonate HPMPC [( S )-1-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine, cidofovir, Vistide ® ] has a unique profile among the antiviral agents in that it is active against a much broader spectrum of DNA viruses than any other antiviral agent, and, furthermore, shows a long-lasting antiviral activity, thus enabling infrequent dosing (for intravenous administration, as infrequent as once a week or every other week). HPMPC owes its antiviral activity to a selective inhibitory effect on viral DNA synthesis: as has been demonstrated for human cytomegalovirus (CMV), HPMPC leads to DNA chain termination following the incorporation of two consecutive HPMPC residues. The activity spectrum of HPMPC encompasses herpes-, adeno-, polyoma-, papilloma-, and poxviruses. It has been approved for the treatment of CMV retinitis in AIDS patients and has proved effective in the treatment of herpes simplex virus (HSV) infections (particularly those that are resistant to acyclovir), human papilloma virus (HPV) infections ( e.g. anogenital warts and recurrent laryngeal papillomatosis) and poxvirus infections ( e.g. molluscum contagiosum). It is now further explored for its therapeutic potential in the treatment of HSV, CMV and HPV infections, and various other DNA virus infections, including adenovirus infections ( e.g. keratoconjunctivitis), polyomavirus infections such as PML (progressive multifocal leukoencephalopathy), poxvirus infections ( e.g. molluscum contagiosum), Epstein-Barr virus (EBV)-associated infections, and human herpesvirus type 8 (HHV-8)-associated infections ( e.g. Kaposi's sarcoma).
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.
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