MK-2048

Systematic (IUPAC) name
MK-2048
(6S)-2-[(3-chloro-4-fluorophenyl)methyl]-8-ethyl-9-hydroxy-N,6-dimethyl-1,10-dioxo-6,7-dihydropyrazino[3,4]pyrrolo[3,4-b]pyridazine-4-carboxamide
Clinical data
Legal status	Investigational New Drug
Identifiers
ATC code	None
PubChem	CID 11554427
ChemSpider	25058456
ChEMBL	CHEMBL1237018
Chemical data
Formula	C₂₁H₂₁ClFN₅O₄
Molar 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 and development)

gp41 (Enfuvirtide (ENF, T-20))
CCR5 (Maraviroc (MVC)
Vicriviroc^†, Cenicriviroc^†, PRO 140^†)
CD4 (Ibalizumab^†)
gp120 (Fostemsavir^†)

Reverse-transcriptase
inhibitors (RTIs)

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

Non-nucleoside (NNRTI) (Discovery and development)	(1st generation) Efavirenz (EFV)°^# Nevirapine (NVP)^# Delavirdine (DLV)^◊ (2nd generation) diarylpyrimidines (Etravirine (ETR) Rilpivirine (RPV)°) Doravirine

Integrase inhibitors
(Integrase strand transfer inhibitors (INSTI))

Dolutegravir (DTG)°
Elvitegravir (EVG)°
Raltegravir (RAL)°
BI 224436^†
Globoidnan A (experimental)
Cabotegravir^†
Bictegravir^†
MK-2048^†

Maturation inhibitors

Bevirimat^†
BMS-955176^§

Protease Inhibitors (PI)
(Discovery and development)

1st generation	Amprenavir (APV)^◊ Fosamprenavir (FPV) Indinavir (IDV)^◊ Lopinavir (LPV) Nelfinavir (NFV) Ritonavir (RTV)^# Saquinavir (SQV)^#

2nd generation	Atazanavir (ATV)°^# Darunavir (DRV)°^# Tipranavir (TPV)

Combined formulations

Abacavir/lamivudine°^#
Abacavir/dolutegravir/lamivudine°
Abacavir/lamivudine/zidovudine
Atazanavir/cobicistat
Darunavir/cobicistat
Efavirenz/emtricitabine/tenofovir°^#
Elvitegravir/cobicistat/emtricitabine/tenofovir°
Emtricitabine/rilpivirine/tenofovir°
Lamivudine/raltegravir
Lamivudine/zidovudine^#
Lopinavir/ritonavir°^#
Tenofovir/emtricitabine°^#

Pharmacokinetic boosters

Experimental agents

Uncoating inhibitors	TRIM5alpha (gene)

Transcription inhibitors	Tat antagonists

Translation inhibitors	Trichosanthin

Other	Abzyme BIT225^† Calanolide A Ceragenin Cyanovirin-N Diarylpyrimidines Epigallocatechin gallate (EGCG) KP-1461^† Foscarnet Fosdevirine^† Griffithsin Hydroxycarbamide 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

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

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

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