Cinacalcet

Calcium-sensing Receptor Agonist — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS

Key facts

Cinacalcet is an ofp drug in the Calcium-sensing Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 2004. Its mechanism of action is classified as Increased Calcium-sensing Receptor Sensitivity. DrugCentral lists 23 molecular targets, including CASR, HTR2B and CYP2D6. Recorded indications include Hypercalcemia due to Primary Hyperparathyroidism, Hyperparathyroidism Secondary to Chronic Renal Failure with Dialysis and Parathyroid Carcinoma with Hypercalcemia.

• Approval status: ofp (first approved 2004 by the FDA).
• Drug class: Calcium-sensing Receptor Agonist.
• Mechanism of action: Increased Calcium-sensing Receptor Sensitivity.
• Molecular targets: CASR, HTR2B, CYP2D6 and SIGMAR1 (23 listed in DrugCentral).
• Indications: Hypercalcemia due to Primary Hyperparathyroidism, Hyperparathyroidism Secondary to Chronic Renal Failure with Dialysis and Parathyroid Carcinoma with Hypercalcemia.
• ATC code: H05BX01 (Other anti-parathyroid agents).
• Molecular formula: C22H22F3N; molecular weight 357.42 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Hypercalcemia due to Primary Hyperparathyroidism
• Hyperparathyroidism Secondary to Chronic Renal Failure with Dialysis
• Parathyroid Carcinoma with Hypercalcemia

Contraindications (7)

• Adynamic bone disease
• Chronic heart failure
• Disease of liver
• Hypocalcemia
• Hypophosphatemia
• Low blood pressure
• Seizure disorder

Mechanism & targets

• Mechanism of action (MoA): Increased Calcium-sensing Receptor Sensitivity
• Established pharmacologic class: Calcium-sensing Receptor Agonist

Molecular targets (23)

Target	Gene	Action	Activity
Extracellular calcium-sensing receptor	CASR	positive allosteric modulator	EC50 7.70
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 7.40
Cytochrome P450 2D6	CYP2D6	unknown	IC50 7.30
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 7.04
Glycine receptor subunit alpha-1	GLRA1	unknown	EC50 6.49
Transmembrane protein 97	TMEM97	unknown	Ki 6.41
D(3) dopamine receptor	DRD3	unknown	Ki 6.41
Kappa-type opioid receptor	OPRK1	unknown	Ki 6.35
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 6.24
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.18
Sodium-dependent serotonin transporter	SLC6A4	unknown	Ki 6.11
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 6.08
5-hydroxytryptamine receptor 5A	HTR5A	unknown	Ki 6.01
Mu-type opioid receptor	OPRM1	unknown	Ki 5.89
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Ki 5.84
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 5.80
5-hydroxytryptamine receptor 1D	HTR1D	unknown	Ki 5.77
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 5.74
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 5.71
Histamine H2 receptor	HRH2	unknown	Ki 5.58

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2004-10-22	EMA	—	—
2004-03-08	FDA	—	AMGEN	Yes

ATC classification

ATC code	Therapeutic hierarchy
H05BX01	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › CALCIUM HOMEOSTASIS › ANTI-PARATHYROID AGENTS › Other anti-parathyroid agents

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Product dose omission issue	17292.4
Hospitalisation	15271.5
Laboratory test abnormal	12309.4
Adverse drug reaction	2174.2
Blood parathyroid hormone increased	2095.2
Intentional product misuse	1636.0
Blood parathyroid hormone abnormal	1185.1
Hypocalcaemia	890.4
Death	840.3
Arteriovenous fistula site complication	732.5
Calciphylaxis	633.2
Unevaluable event	623.5

Chemical structure

• Molecular formula: C₂₂H₂₂F₃N
• Molecular weight: 357.42 g/mol
• CAS number: 226256-56-0
• InChIKey: VDHAWDNDOKGFTD-MRXNPFEDSA-N
• PubChem CID: 156419

C[C@@H](NCCCC1=CC(=CC=C1)C(F)(F)F)C1=CC=CC2=C1C=CC=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Cinacalcet used for?

DrugCentral lists the following indications for Cinacalcet: Hypercalcemia due to Primary Hyperparathyroidism, Hyperparathyroidism Secondary to Chronic Renal Failure with Dialysis and Parathyroid Carcinoma with Hypercalcemia.

How does Cinacalcet work?

Cinacalcet is classified as Increased Calcium-sensing Receptor Sensitivity; its molecular targets in DrugCentral include CASR (positive allosteric modulator), HTR2B, CYP2D6 and SIGMAR1.

When was Cinacalcet first approved?

Cinacalcet was first approved by the FDA in 2004.

What drug class does Cinacalcet belong to?

Cinacalcet is in the Calcium-sensing Receptor Agonist class.

What is the chemical formula of Cinacalcet?

Cinacalcet has the molecular formula C22H22F3N and a molecular weight of 357.42 g/mol.

Sources

• DrugCentral drug card 647 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200776 — compound record and bioactivity
• PubChem CID 156419 — chemical identifiers
• DrugBank DB01012 — drug record
• FDA UNII UAZ6V7728S — substance identity
• DailyMed: FDA labels for Cinacalcet — current prescribing information (label search)
• UniProt P41180 (CASR) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt P10635 (CYP2D6) — target protein
• UniProt Q99720 (SIGMAR1) — target protein
• UniProt P23415 (GLRA1) — target protein
• UniProt Q5BJF2 (TMEM97) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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