Doravirine

Doravirine
Clinical data
Trade names	Pifeltro
Synonyms	MK-1439
Routes of; administration	Oral[1]
ATC code	none;
Legal status
Legal status	US: ℞-only ;
Identifiers
	IUPAC name 3-Chloro-5-({1-[(4-methyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)-1,2-dihydro-3-pyridinyl}oxy)benzonitrile;
CAS Number	1338225-97-0;
PubChem CID	58460047;
ChemSpider	28424197;
UNII	913P6LK81M;
KEGG	D10624;
ChEMBL	CHEMBL2364608;
PDB ligand	2KW (PDBe, RCSB PDB);
ECHA InfoCard	100.234.454
Chemical and physical data
Formula	C17H11ClF3N5O3
Molar mass	425.75 g/mol
3D model (JSmol)	Interactive image;
	SMILES Cn1c(n[nH]c1=O)Cn2ccc(c(c2=O)Oc3cc(cc(c3)Cl)C#N)C(F)(F)F;
	InChI InChI=1S/C17H11ClF3N5O3/c1-25-13(23-24-16(25)28)8-26-3-2-12(17(19,20)21)14(15(26)27)29-11-5-9(7-22)4-10(18)6-11/h2-6H,8H2,1H3,(H,24,28); Key:ZIAOVIPSKUPPQW-UHFFFAOYSA-N;

Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor developed by Merck & Co. for use in the treatment of HIV/AIDS. Doravirine demonstrated robust antiviral activity and good tolerability in a small clinical study of 7-day monotherapy reported at the 20th Conference on Retroviruses and Opportunistic Infections in March 2013. Doravirine appeared safe and generally well-tolerated with most adverse events being mild-to-moderate.^[2]^[3] In August 2018, the FDA approved doravine under the product name Pifeltro, and in a combination tablet, doravirine/lamivudine/tenofovir disoproxil fumarate (Delstrigo).^[4]

References

↑ Collins, Simon; Horn, Tim. "The Antiretroviral Pipeline" (PDF). Pipeline Report. p. 10. Archived from the original (PDF) on 11 March 2016. Retrieved 6 December 2015.
↑ Safety and Antiviral Activity of MK-1439, a Novel NNRTI, in Treatment-naïve HIV+ Patients. Gathe, Joseph et al. 20th Conference on Retroviruses and Opportunistic Infections. 3–6 March 2013. Abstract 100.
↑ CROI 2013: MK-1439, a Novel HIV NNRTI, Shows Promise in Early Clinical Trials. Highleyman, Liz. HIVandHepatitis.com. 6 March 2013.
↑ FDA Approves Merck’s DELSTRIGO™ (doravirine / lamivudine / tenofovir disoproxil fumarate), a Once-Daily Fixed-Dose Combination Tablet as a Complete Regimen and PIFELTRO™ (doravirine), an NNRTI, Both for the Treatment of HIV-1 in Appropriate Patients

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[1] Collins, Simon; Horn, Tim. "The Antiretroviral Pipeline" (PDF). Pipeline Report. p. 10. Archived from the original (PDF) on 11 March 2016. Retrieved 6 December 2015.

[2] Safety and Antiviral Activity of MK-1439, a Novel NNRTI, in Treatment-naïve HIV+ Patients. Gathe, Joseph et al. 20th Conference on Retroviruses and Opportunistic Infections. 3–6 March 2013. Abstract 100.

[3] CROI 2013: MK-1439, a Novel HIV NNRTI, Shows Promise in Early Clinical Trials. Highleyman, Liz. HIVandHepatitis.com. 6 March 2013.

[4] FDA Approves Merck’s DELSTRIGO™ (doravirine / lamivudine / tenofovir disoproxil fumarate), a Once-Daily Fixed-Dose Combination Tablet as a Complete Regimen and PIFELTRO™ (doravirine), an NNRTI, Both for the Treatment of HIV-1 in Appropriate Patients