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Diarylpyrimidines

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Diarylpyrimidines

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Chemical structure of etravirine (Intelence)

Diarylpyrimidines (DAPY) and diaryltriazines (DATA) are two closely related classes of molecules resembling the pyrimidine nucleotides found in DNA. They show great potency in inhibiting the activity of HIV reverse transcriptase. Several compounds in this class are non-nucleoside reverse transcriptase inhibitors used clinically in the treatment of HIV/AIDS, notably etravirine and rilpivirine.

Entry/fusion inhibitors
(Discovery and development)

Integrase inhibitors
(Integrase strand transfer inhibitors (INSTI))

Protease Inhibitors (PI)
(Discovery and development)

1^st generation	Amprenavir (APV)^‡ Fosamprenavir (FPV) Indinavir (IDV)^◊ Lopinavir (LPV) Nelfinavir (NFV)^◊ Ritonavir (RTV)^# Saquinavir (SQV)^◊
2^nd generation	Atazanavir (ATV)°^# Darunavir (DRV)°^# Tipranavir (TPV)^◊ TMC-310911^§

Non-nucleoside (NNRTI)
(Discovery and development)

1^st generation	Efavirenz (EFV)^# Nevirapine (NVP)^# Delavirdine (DLV)^‡
2^nd generation	diarylpyrimidines Etravirine (ETR) Rilpivirine (RPV) Doravirine (DOR)

Pharmacokinetic boosters

Experimental agents

Uncoating inhibitors	TRIM5alpha (gene)
Transcription inhibitors	Tat antagonists
Translation inhibitors	Trichosanthin
BNAbs	Elipovimab
Other	Abzyme BIT225^† Calanolide A Ceragenin Cyanovirin-N Diarylpyrimidines Epigallocatechin gallate (EGCG) Foscarnet Fosdevirine^† Griffithsin Hydroxycarbamide KP-1461^† Miltefosine Portmanteau inhibitors Scytovirin Seliciclib^† Synergistic enhancers Tre recombinase Zinc finger protein transcription factor
Failed agents	Aplaviroc Atevirdine Brecanavir Capravirine Dexelvucitabine Droxinavir Lasinavir Emivirine Lersivirine Lodenosine Loviride Mozenavir Palinavir Telinavir

°DHHS recommended initial regimen options. ^◊Formerly or rarely used agent.