Lorundrostat

Lorundrostat
Clinical data
Other names	MLS 101
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name N-(4-Acetamidocyclohexyl)-2-[4-[5-(4-methylphenyl)-1,2,4-triazin-3-yl]piperazin-1-yl]acetamide;
CAS Number	1820940-17-7;
PubChem CID	126567187;
ChemSpider	123963150;
UNII	KA8W5LDS6Z;
KEGG	D12773;
ChEMBL	ChEMBL5095105;
Chemical and physical data
Formula	C24H33N7O2
Molar mass	451.575 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=CC=C(C=C1)C2=CN=NC(=N2)N3CCN(CC3)CC(=O)NC4CCC(CC4)NC(=O)C;
	InChI InChI=1S/C24H33N7O2/c1-17-3-5-19(6-4-17)22-15-25-29-24(28-22)31-13-11-30(12-14-31)16-23(33)27-21-9-7-20(8-10-21)26-18(2)32/h3-6,15,20-21H,7-14,16H2,1-2H3,(H,26,32)(H,27,33); Key:YHGVDZULVMINCJ-UHFFFAOYSA-N;

Short description: Chemical compound

Lorundrostat (developmental name MLS 101) is an aldosterone synthase inhibitor developed by Mineralys Therapeutics for high blood pressure. In clinical trials as an add-on medication for people with uncontrolled hypertension, decreased renin and elevated aldosterone it significantly reduced blood pressure. Hyperkalemia occurred in some trial participants.^[1]^[2]^[3]^[4]

References

↑ Laffin, Luke J.; Rodman, David; Luther, James M.; Vaidya, Anand; Weir, Matthew R.; Rajicic, Natasa; Slingsby, B. T.; Nissen, Steven E. et al. (26 September 2023). "Aldosterone Synthase Inhibition With Lorundrostat for Uncontrolled Hypertension: The Target-HTN Randomized Clinical Trial" (in en). JAMA 330 (12): 1140–1150. doi:10.1001/jama.2023.16029. ISSN 0098-7484. PMID 37690061.
↑ Rodman, David; Weir, Matthew R.; Slingsby, Bt; Laffin, Luke; Nissen, Steven E. (March 2023). "Highly Effective Blood Pressure Lowering with MLS-101, A New Aldosterone Synthase Inhibitor, in Individuals with Obesity and Raas Dysregulation" (in en). Journal of the American College of Cardiology 81 (8): 306. doi:10.1016/S0735-1097(23)00750-7. https://www.jacc.org/doi/full/10.1016/S0735-1097%2823%2900750-7.
↑ Fujii, Aya; Hiraga, Yuki; Kawai, Mizue; Ogawa, Kei; Ohta, Yoshiyasu; Rahman, Sheikh Mohammed Ashfaq; Shimizu, Hidetoshi; Sugimoto-Kawabata, Kanami et al. (March 2023). "First-In-Human Study of MLS-101, A Potent and Highly Selective Aldosterone Synthase Inhibitor" (in en). Journal of the American College of Cardiology 81 (8): 616. doi:10.1016/S0735-1097(23)01060-4. https://www.jacc.org/doi/full/10.1016/S0735-1097%2823%2901060-4.
↑ Irfan, Hamza; Ahmed, Aliza; Nawani, Komal Devi (January 2024). "Hypertension and Lorundrostat: Key Discoveries From the TARGET-HTN Trial". Current Problems in Cardiology 49 (1): 102144. doi:10.1016/j.cpcardiol.2023.102144. PMID 37858848.

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[1] Laffin, Luke J.; Rodman, David; Luther, James M.; Vaidya, Anand; Weir, Matthew R.; Rajicic, Natasa; Slingsby, B. T.; Nissen, Steven E. et al. (26 September 2023). "Aldosterone Synthase Inhibition With Lorundrostat for Uncontrolled Hypertension: The Target-HTN Randomized Clinical Trial" (in en). JAMA 330 (12): 1140–1150. doi:10.1001/jama.2023.16029. ISSN 0098-7484. PMID 37690061.

[2] Rodman, David; Weir, Matthew R.; Slingsby, Bt; Laffin, Luke; Nissen, Steven E. (March 2023). "Highly Effective Blood Pressure Lowering with MLS-101, A New Aldosterone Synthase Inhibitor, in Individuals with Obesity and Raas Dysregulation" (in en). Journal of the American College of Cardiology 81 (8): 306. doi:10.1016/S0735-1097(23)00750-7. https://www.jacc.org/doi/full/10.1016/S0735-1097%2823%2900750-7.

[3] Fujii, Aya; Hiraga, Yuki; Kawai, Mizue; Ogawa, Kei; Ohta, Yoshiyasu; Rahman, Sheikh Mohammed Ashfaq; Shimizu, Hidetoshi; Sugimoto-Kawabata, Kanami et al. (March 2023). "First-In-Human Study of MLS-101, A Potent and Highly Selective Aldosterone Synthase Inhibitor" (in en). Journal of the American College of Cardiology 81 (8): 616. doi:10.1016/S0735-1097(23)01060-4. https://www.jacc.org/doi/full/10.1016/S0735-1097%2823%2901060-4.

[4] Irfan, Hamza; Ahmed, Aliza; Nawani, Komal Devi (January 2024). "Hypertension and Lorundrostat: Key Discoveries From the TARGET-HTN Trial". Current Problems in Cardiology 49 (1): 102144. doi:10.1016/j.cpcardiol.2023.102144. PMID 37858848.

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Lorundrostat

Topic: Chemistry

References