Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMQSPFS)

Drug Name

Encaleret Drug Info

Synonyms

ENCALERET; 787583-71-5; EF8081AQ6G; CHEMBL1672973; Encaleret (USAN); ENCALERET [USAN]; 2'-((1R)-1-(((1-(4-chloro-3-fluorophenyl)-2-methylpropan-2-yl)amino)-(2R)-2-hydroxypropoxy)ethyl)-3-methyl(1,1'-biphenyl)-4-carboxylic acid; 2'-((1R)-1-(((2R)-3-((1-(4-chloro-3-fluorophenyl)-2-methylpropan-2-yl)amino)-2-hydroxypropyl)oxy)ethyl)-3-methyl-1,1'-biphenyl-4-carboxylic acid; Encaleret [INN]; (1,1'-Biphenyl)-4-carboxylic acid, 2'-((1R)-1-((2R)-3-((2-(4-chloro-3-fluorophenyl)-1,1-dimethylethyl)amino)-2-hydroxypropoxy)ethyl)-3-methyl-; Encaleret [USAN:INN]; UNII-EF8081AQ6G; ENCALERET [WHO-DD]; CLTX305; SCHEMBL482046; CLTX-305; GTPL9474; BDBM50337103; AKOS040751679; 4-[2-[(1R)-1-[(2R)-3-[[1-(4-chloro-3-fluorophenyl)-2-methylpropan-2-yl]amino]-2-hydroxypropoxy]ethyl]phenyl]-2-methylbenzoic acid; D10068; Q27277151; 2''-((1R)-1-{(2R)-3-[1-(4-Chloro-3-fluorophenyl)-2-methylpropan-2-ylamino]-2-hydroxypropoxy}ethyl)-3-methylbiphenyl-4-carboxylic acid hemisulfate; 2'-((1R)-1-((2R)-3-((1-(4-CHLORO-3-FLUOROPHENYL)-2-METHYLPROPAN-2-YL)AMINO)-2-HYDROXYPROPOXY)ETHYL)-3-METHYL(1,1'-BIPHENYL)-4-CARBOXYLIC ACID

Indication

Disease Entry	ICD 11	Status	REF
Autosomal dominant hypocalcemia	5A50.0Y	Phase 3	[1]

Cross-matching ID

PubChem CID: 46917559
TTD Drug ID: DMQSPFS

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Preclinical Drug(s)

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Drug(s) Targeting Extracellular calcium-sensing receptor (CASR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cinacalcet	DMCX0K3	Hyperparathyroidism	5A51	Approved	[3]
Etelcalcetide	DMHP9BL	Secondary hyperparathyroidism	5A51.1	Approved	[4]
ASP7991	DM3TN1A	Hyperparathyroidism	5A51	Phase 2	[5]
MK-5442	DMHTIGU	Osteoporosis	FB83.0	Phase 2	[6]
ATF-936	DMWGKHZ	Osteoporosis	FB83.0	Phase 1	[7]
AXT-914	DM7ZU3B	Osteoporosis	FB83.0	Phase 1	[8]
R-568	DM5NWPD	N. A.	N. A.	Discontinued in Phase 2	[9]
Ronacaleret	DM10ZJP	Osteoporosis	FB83.0	Discontinued in Phase 2	[10]
NPS-2143	DMQPXLF	Osteoporosis	FB83.0	Discontinued in Phase 2	[11]
NPS-2390	DMMRY0Z	Cerebrovascular ischaemia	8B1Z	Preclinical	[12]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Extracellular calcium-sensing receptor (CASR)	TTBUYHA	CASR_HUMAN	Antagonist	[2]

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References

1	ClinicalTrials.gov (NCT05680818) CALIBRATE: A Phase 3, Randomized, Open-Label Study Evaluating the Efficacy and Safety of Encaleret Compared to Standard of Care in Participants With Autosomal Dominant Hypocalcemia Type 1 (ADH1). U.S.National Institutes of Health.
2	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
3	Clinical pipeline report, company report or official report of Amgen (2009).
4	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035616)
6	Antagonist for calcium-sensing receptor. JTT-305/MK-5442. Clin Calcium. 2011 Jan;21(1):89-93.
7	ATF936, a novel oral calcilytic, increases bone mineral density in rats and transiently releases parathyroid hormone in humans. Bone. 2011 Aug;49(2):233-41.
8	AXT914 a novel, orally-active parathyroid hormone-releasing drug in two early studies of healthy volunteers and postmenopausal women. Bone. 2014 Jul;64:204-10.
9	Mixed-effects modeling of the pharmacodynamic response to the calcimimetic agent R-568. Clin Pharmacol Ther. 1999 Jan;65(1):40-9.
10	Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
11	Calcium-sensing receptor antagonist (calcilytic) NPS 2143 specifically blocks the increased secretion of endogenous Abeta42 prompted by exogenous fibrillary or soluble Abeta25-35 in human cortical astrocytes and neurons-therapeutic relevance to Alzheimer's disease. Biochim Biophys Acta. 2013 Oct;1832(10):1634-52.
12	The Extracellular Calcium-Sensing Receptor (CASR) Regulates Gonadotropins-Induced Meiotic Maturation of Porcine Oocytes.Biol Reprod.2015 Dec;93(6):131.