Desidustat

Desidustat
Clinical data
Synonyms	ZYAN1
Identifiers
	IUPAC name 2-[[1-(Cyclopropylmethoxy)-4-hydroxy-2-oxoquinoline-3-carbonyl]amino]acetic acid;
CAS Number	1616690-16-4;
UNII	Y962PQA4KS;
Chemical and physical data
Formula	C16H16N2O6
Molar mass	332.31 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CC1CON2C3=CC=CC=C3C(=C(C2=O)C(=O)NCC(=O)O)O;
	InChI InChI=1S/C16H16N2O6/c19-12(20)7-17-15(22)13-14(21)10-3-1-2-4-11(10)18(16(13)23)24-8-9-5-6-9/h1-4,9,21H,5-8H2,(H,17,22)(H,19,20); Key:IKRKQQLJYBAPQT-UHFFFAOYSA-N;

Desidustat (INN, also known as ZYAN1) is an investigational drug for the treatment of anemia of chronic kidney disease. Clinical trials on desidustat have been done in India and Australia.^[1] It is currently undergoing Phase 2 clinical trials.^[2] Desidustat is being developed for the treatment of anemia, where currently erythropoietin and its analogues are drugs of choice. Desidustat is a prolyl hydroxylase domain (PHD) inhibitor. In preclinical studies, effect of desidustat was assessed in normal and nephrectomized rats, and in chemotherapy-induced anemia. Desidustat demonstrated hematinic potential by combined effects on endogenous erythropoietin release and efficient iron utilization.^[3]^[4]

References

↑ Kansagra, Kevinkumar A.; Parmar, Deven; Jani, Rajendra H.; Srinivas, Nuggehally R.; Lickliter, Jason; Patel, Harilal V.; Parikh, Devang P.; Heading, Heather; Patel, Hardik B.; Gupta, Rahul J.; Shah, Chintan Y.; Patel, Maulik R.; Dholakia, Vyom N.; Sukhadiya, Raghav; Jain, Mukul R.; Parmar, Krupi V.; Barot, Kinjal (16 May 2017). "Phase I Clinical Study of ZYAN1, A Novel Prolyl-Hydroxylase (PHD) Inhibitor to Evaluate the Safety, Tolerability, and Pharmacokinetics Following Oral Administration in Healthy Volunteers". Clinical Pharmacokinetics. doi:10.1007/s40262-017-0551-3. PMID 28508936.
↑ "Zydus starts phase II trials of molecule targeting anaemia". 5 July 2017. Retrieved 9 December 2017 – via The Economic Times.
↑ Jain, M.; Joharapurkar, A.; Pandya, V.; Patel, V.; Joshi, J.; Kshirsagar, S.; Patel, K.; Patel, P.; Desai, R. (14 September 2015). "Pharmacological Characterization of ZYAN1, a Novel Prolyl Hydroxylase Inhibitor for the Treatment of Anemia". Drug Research. 66 (02): 107–112. doi:10.1055/s-0035-1554630. PMID 26367279.
↑ Joharapurkar AA, Pandya VB, Patel VJ, Desai RC, Jain MR.Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.J Med Chem. 2018 May 9. doi: 10.1021/acs.jmedchem.7b01686.

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[1] Kansagra, Kevinkumar A.; Parmar, Deven; Jani, Rajendra H.; Srinivas, Nuggehally R.; Lickliter, Jason; Patel, Harilal V.; Parikh, Devang P.; Heading, Heather; Patel, Hardik B.; Gupta, Rahul J.; Shah, Chintan Y.; Patel, Maulik R.; Dholakia, Vyom N.; Sukhadiya, Raghav; Jain, Mukul R.; Parmar, Krupi V.; Barot, Kinjal (16 May 2017). "Phase I Clinical Study of ZYAN1, A Novel Prolyl-Hydroxylase (PHD) Inhibitor to Evaluate the Safety, Tolerability, and Pharmacokinetics Following Oral Administration in Healthy Volunteers". Clinical Pharmacokinetics. doi:10.1007/s40262-017-0551-3. PMID 28508936.

[2] "Zydus starts phase II trials of molecule targeting anaemia". 5 July 2017. Retrieved 9 December 2017 – via The Economic Times.

[3] Jain, M.; Joharapurkar, A.; Pandya, V.; Patel, V.; Joshi, J.; Kshirsagar, S.; Patel, K.; Patel, P.; Desai, R. (14 September 2015). "Pharmacological Characterization of ZYAN1, a Novel Prolyl Hydroxylase Inhibitor for the Treatment of Anemia". Drug Research. 66 (02): 107–112. doi:10.1055/s-0035-1554630. PMID 26367279.

[4] Joharapurkar AA, Pandya VB, Patel VJ, Desai RC, Jain MR.Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.J Med Chem. 2018 May 9. doi: 10.1021/acs.jmedchem.7b01686.