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Imidafenacin

Imidafenacin structure

CAS No:
170105-16-5
Formula:
C20H21N3O
Chemical Name:
Imidafenacin
Synonyms:
1H-Imidazole-1-butanamide,2-methyl-α,α-diphenyl-;2-Methyl-α,α-diphenyl-1H-imidazole-1-butanamide;KRP 197;4-(2-Methyl-1-imidazolyl)-2,2-diphenylbutanamide;Imidafenacin;ONO 8025;Staybla;Uritos;4-(2-Methyl-1H-imidazol-1-yl)-2,2-diphenylbutanamide
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Imidafenacin is a diarylmethane.|Imidafenacin is an antispasmodic agent with anticholinergic effects. It antagonizes muscarinic receptors in the bladder to reduce the frequency of urination in the treatment of overactive bladder. It is marketed in Japan under the tradenames Staybla by Ono Pharmaceutical and Uritos by Kyojin Pharmaceutical.

Imidafenacin Basic Attributes

Molecular Weight：

319.40000

Exact Mass：

319.40

UNII：

XJR8Y07LJO

Characteristics

PSA：

61.90000

XLogP3：

4.20290

Density：

1.12g/cm3

Boiling Point：

579.7ºC at 760mmHg

Flash Point：

304.4ºC

Refractive Index：

1.602

Vapor Pressure：

1.96E-13mmHg at 25°C

Safety Information

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 2 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Toxicity Summary：

Clinically significant adverse reactions to imidafenacin are acute glaucoma (0.06%), urinary retention (0.03%), and heptic dysfunction (0.02%). The most common adverse effects observed with imidafenacin are thirst (37.7%), constipation (13.6%).

Protein Binding：

Imidafenacin is 88% bounf by human plasma proteins. It binds to serum albumin and α1-acid glycoprotein.

Drug Information

Drug Indication：

Used in the treatment of overactive bladder.|FDA Label

Pharmacology：

Imidafenacin is an antimuscarinic agent which acts to reduce the frequency of urination in patients with overactive bladder.

Absorption：

The absolute oral bioavailability is 57.8%. Tmax is 1-3 h after administration.|10% is excreted in the urine as the parent compound. Most is eliminated by metabolism thought to be mediated by CYP3A4 and UGT1A4.|The estimated volume of distribution is 43.9 L.|The estimated clearance is 21.2 L/h.

Metabolism/Metabolites：

Thought to be metabolized v by CYP3A4 and UGT1A4. No active metabolites have been observed.

Biological Half-Life：

The half life of elimination is 3 h.

Mechanism of Action：

Imidafenacin binds to and antagonizes muscarinic M1 and M3 receptors with high affinity. It also antagonizes muscarinic M2 receptors but with lower affinity. M3 receptors stimulate contraction of the detrusor muscle in the bladder via release of calcium from the sarcoplasmic reticulum. M2 receptors are also present in the detrusor muscle but serve to inhibit adenylate cyclase which reduces the relaxation mediated by β adrenergic receptors. Finally, M1 receptors are present on the parasympathetic neurons which release acetylcholine in the bladder. They act as an autocrine positive feedback loop and further increase release of acetylcholine. Antagonism of these receptors by imidafenacin prevents contraction of the bladder's detrusor muscle, prevents inhibition of the relation produced by sympathetic tone, and reduces acetylcholine release. Together these reduce the frequency of urination.

MeSH Entry Terms：

imidafenacin

Computed Properties

Molecular Weight:319.4
XLogP3:2.7
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:6
Exact Mass:319.168462302
Monoisotopic Mass:319.168462302
Topological Polar Surface Area:60.9
Heavy Atom Count:24
Complexity:395
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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