N-0385

N-0385
Clinical data
Other names	Ms-QFR-Kbt
Routes of; administration	Intranasal
Identifiers
	IUPAC name (2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-(methanesulfonamido)pentanediamide;
PubChem CID	135169285;
IUPHAR/BPS	11956;
Chemical and physical data
Formula	C28H36N8O6S2
Molar mass	644.77 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CS(=O)(=O)NC(CCC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCN=C(N)N)C(=O)C2=NC3=CC=CC=C3S2;
	InChI InChI=1S/C28H36N8O6S2/c1-44(41,42)36-20(13-14-23(29)37)25(39)34-21(16-17-8-3-2-4-9-17)26(40)33-19(11-7-15-32-28(30)31)24(38)27-35-18-10-5-6-12-22(18)43-27/h2-6,8-10,12,19-21,36H,7,11,13-16H2,1H3,(H2,29,37)(H,33,40)(H,34,39)(H4,30,31,32)/t19-,20-,21-/m0/s1; Key:JTHVOFMYRRNGPA-ACRUOGEOSA-N;

N-0385 is an experimental small molecule TMPRSS2-inhibitor being investigated for its potential use in the prevention and treatment of COVID-19.^[1]^[2]^[3]^[4]^[5]

Mechanism of action

N-0385 is thought to have antiviral effects by targeting key proteins involved in the viral entry process, including TMPRSS2, ACE2, and DPP4. By interfering with the interactions between these proteins and the SARS-CoV-2 spike protein, N-0385 effectively blocks the virus from gaining access to host cells.^[3]^[4]^[5] Additionally, N-0385 appears to modify the immune responses and inflammatory pathways associated with the infection by regulating TLR7, NLRP3, and IL-10, potentially reducing the severity of COVID-19 symptoms and reducing tissue damage associated with the infection.^[4]

References

^ Sankaran, Vishwam (30 March 2022). "New nasal spray found 'effective' in preventing and treating Covid in mice". The Independent. Retrieved 16 November 2023.
^ Reynolds, Sharon (11 April 2022). "Nasal antiviral blocks SARS-CoV-2 infection in mice". Institutes of Health (NIH). Retrieved 16 November 2023.
^ ^a ^b Shapira T, Monreal IA, Dion SP, Buchholz DW, Imbiakha B, Olmstead AD, Jager M, Désilets A, Gao G, Martins M, Vandal T, Thompson C, Chin A, Rees WD, Steiner T, Nabi IR, Marsault E, Sahler J, Diel DG, Van de Walle GR, August A, Whittaker GR, Boudreault PL, Leduc R, Aguilar HC, Jean F (May 2022). "A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic". Nature. 605 (7909): 340–348. Bibcode:2022Natur.605..340S. doi:10.1038/s41586-022-04661-w. PMC 9095466. PMID 35344983.
^ ^a ^b ^c Cao JF, Yang X, Xiong L, Wu M, Chen S, Xiong C, He P, Zong Y, Zhang L, Fu H, Qi Y, Ying X, Liu D, Hu X, Zhang X (October 2022). "Mechanism of N-0385 blocking SARS-CoV-2 to treat COVID-19 based on molecular docking and molecular dynamics". Frontiers in Microbiology. 13. doi:10.3389/fmicb.2022.1013911. PMC 9622768. PMID 36329841.
^ ^a ^b Pérez-Vargas J, Lemieux G, Thompson CA, Désilets A, Ennis S, Gao G, Gordon DG, Schulz AL, Niikura M, Nabi IR, Krajden M, Boudreault PL, Leduc R, Jean F (May 2024). "Nanomolar anti-SARS-CoV-2 Omicron activity of the host-directed TMPRSS2 inhibitor N-0385 and synergistic action with direct-acting antivirals". Antiviral Research. 225: 105869. doi:10.1016/j.antiviral.2024.105869. PMID 38548023.

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[Sankaran_2022-1] Sankaran, Vishwam (30 March 2022). "New nasal spray found 'effective' in preventing and treating Covid in mice". The Independent. Retrieved 16 November 2023.

[Reynolds_2022-2] Reynolds, Sharon (11 April 2022). "Nasal antiviral blocks SARS-CoV-2 infection in mice". Institutes of Health (NIH). Retrieved 16 November 2023.

[pmid35344983-3] Shapira T, Monreal IA, Dion SP, Buchholz DW, Imbiakha B, Olmstead AD, Jager M, Désilets A, Gao G, Martins M, Vandal T, Thompson C, Chin A, Rees WD, Steiner T, Nabi IR, Marsault E, Sahler J, Diel DG, Van de Walle GR, August A, Whittaker GR, Boudreault PL, Leduc R, Aguilar HC, Jean F (May 2022). "A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic". Nature. 605 (7909): 340–348. Bibcode:2022Natur.605..340S. doi:10.1038/s41586-022-04661-w. PMC 9095466. PMID 35344983.

[pmid36329841-4] Cao JF, Yang X, Xiong L, Wu M, Chen S, Xiong C, He P, Zong Y, Zhang L, Fu H, Qi Y, Ying X, Liu D, Hu X, Zhang X (October 2022). "Mechanism of N-0385 blocking SARS-CoV-2 to treat COVID-19 based on molecular docking and molecular dynamics". Frontiers in Microbiology. 13. doi:10.3389/fmicb.2022.1013911. PMC 9622768. PMID 36329841.

[pmid38548023-5] Pérez-Vargas J, Lemieux G, Thompson CA, Désilets A, Ennis S, Gao G, Gordon DG, Schulz AL, Niikura M, Nabi IR, Krajden M, Boudreault PL, Leduc R, Jean F (May 2024). "Nanomolar anti-SARS-CoV-2 Omicron activity of the host-directed TMPRSS2 inhibitor N-0385 and synergistic action with direct-acting antivirals". Antiviral Research. 225: 105869. doi:10.1016/j.antiviral.2024.105869. PMID 38548023.

[1]

[2]

[3]

[4]

[5]

Clinical data

Other names	Ms-QFR-Kbt
Routes of administration	Intranasal
Identifiers
IUPAC name (2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-(methanesulfonamido)pentanediamide
PubChem CID	135169285
IUPHAR/BPS	11956
Chemical and physical data
Formula	C₂₈H₃₆N₈O₆S₂
Molar mass	644.77 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CS(=O)(=O)NC(CCC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CCCN=C(N)N)C(=O)C2=NC3=CC=CC=C3S2
InChI InChI=1S/C28H36N8O6S2/c1-44(41,42)36-20(13-14-23(29)37)25(39)34-21(16-17-8-3-2-4-9-17)26(40)33-19(11-7-15-32-28(30)31)24(38)27-35-18-10-5-6-12-22(18)43-27/h2-6,8-10,12,19-21,36H,7,11,13-16H2,1H3,(H2,29,37)(H,33,40)(H,34,39)(H4,30,31,32)/t19-,20-,21-/m0/s1 Key:JTHVOFMYRRNGPA-ACRUOGEOSA-N