MK-2048

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MK-2048

Systematic (IUPAC) name
(6S)-2-(3-chloro-4-fluorobenzyl)-8-ethyl-10-hydroxy-N,6-dimethyl-1,9-dioxo-1,2,6,7,8,9-hexahydropyrazino‌[1′,2′:1,5]‌pyrrolo‌[2,3-d]‌pyridazine-4-carboxamide
Clinical data
Legal status	Investigational
Identifiers

ATC code	None
PubChem	CID 11554427
ChEMBL	CHEMBL1237018
Chemical data
Formula	C₂₁H₂₁Cl F N₅O₄
Mol. mass	461.87 g/mol
SMILES CCN1CC(N2C3=C(C(=O)C2=C1O)C(=O)N(N=C3C(=O)NC)CC4=CC(=C(C=C4)F)Cl)C
InChI InChI=1S/C21H21ClFN5O4/c1-4-26-8-10(2)28-16-14(18(29)17(28)21(26)32)20(31)27(25-15(16)19(30)24-3)9-11-5-6-13(23)12(22)7-11/h5-7,10,32H,4,8-9H2,1-3H3,(H,24,30)/t10-/m0/s1 Key:IOYLKNABOQYKKY-JTQLQIEISA-N

MK-2048 is a second generation integrase inhibitor, intended to be used against HIV infection. It is superior to the first available integrase inhibitor, raltegravir, in that it inhibits the HIV enzyme integrase 4 times longer. It is being investigated for use as part of pre-exposure prophylaxis (PrEP). ^[1]

It is being developed by Merck & Co.^[2]

References

↑ Keith Alcorn. Ralvetgravir shows potential for use as PrEP drug AIDSmap.com. 28 April 2009. Accessed 8 Nov 2009.
↑ Mark Mascolini. Merck Offers Unique Perspective on Second-Generation Integrase Inhibitor. 10th International Workshop on Clinical Pharmacology of HIV Therapy, April 15–17, 2009, Amsterdam. Accessed 8 Nov 2009.

Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)

Entry/fusion inhibitors
(Discovery & development)

gp41 (Enfuvirtide)
CCR5 (Maraviroc
Vicriviroc^†, Cenicriviroc^†, PRO 140^†)
CD4 (Ibalizumab^†)

Reverse-transcriptase
inhibitors (RTIs)

Nucleoside & nucleotide (NRTI)	Nucleoside analogues/NARTIs: Abacavir (ABC)°^# Emtricitabine (FTC)°^# Lamivudine (3TC)°^# Didanosine (ddI)^# Zidovudine (AZT)^# Apricitabine^† Stampidine^† Elvucitabine^† Racivir^† Amdoxovir^† Stavudine (d4T)^# Zalcitabine (ddC)^◊ Festinavir^† Nucleotide analogues/NtRTIs: Tenofovir disoproxil fumarate (TDF)°^# Tenofovir alafenamide fumarate (TAF)^†

Non-nucleoside (NNRTI) (Discovery & development)	(1st generation) Efavirenz (EFV)°^# Nevirapine (NVP)^# Loviride^◊ Delavirdine (DLV)^◊ (2nd generation) diarylpyrimidines (Etravirine Rilpivirine) Lersivirine^†

Integrase inhibitors

Maturation inhibitors

Bevirimat^†

Protease Inhibitors (PI)
(Discovery and development)

1st generation	Fosamprenavir° Lopinavir°^# Nelfinavir^# Ritonavir^# Saquinavir^# Amprenavir^◊ Indinavir^◊^#

2nd generation	Atazanavir° Darunavir° Tipranavir

Combined formulations

Experimental agents

Uncoating inhibitors	TRIM5alpha (gene)

Transcription inhibitors	Tat antagonists

Translation inhibitors	Trichosanthin

Other	Abzyme Calanolide A Ceragenin Cyanovirin-N Diarylpyrimidines Epigallocatechin gallate (EGCG) Foscarnet Griffithsin Hydroxycarbamide Miltefosine Portmanteau inhibitors Seliciclib^† Synergistic enhancers Tre recombinase Zinc finger protein transcription factor KP-1461^† Cobicistat^†

Failed agents	Dexelvucitabine Capravirine Emivirine Lodenosine Atevirdine Brecanavir Aplaviroc

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

°DHHS preferred first-line agent. ^◊Formerly or rarely used agent.

M: VIR

virs(prot)/clss

cutn/syst (hppv/hiva, infl/zost/zoon)/epon

drug (dnaa, rnaa, rtva, vacc)

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