Vonoprazan fumarate

China [CN]

I. Basic Information

Item | Details

English Name | Vonoprazan fumarate; Takecab (trade name)

Chinese Name | Vonoprazan fumarate

CAS Number | 1260141-27-2 (fumarate); 1026256-79-0 (free base)

Chemical Name | 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (1:1)

Molecular Formula | Free base C₁₇H₁₆FN₃O₂S; Fumarate C₁₇H₁₆FN₃O₂S・C₄H₄O₄

Molecular Weight | Free base 345.39; Fumarate 465.49

Target | Gastric parietal cell H⁺/K⁺-ATPase (potassium ion binding site)

Developer | Takeda Pharmaceutical Company Limited (Japan)

Market Launch Date | December 2014 (Japan); April 2022 (China NMPA)

Dosage Form and Strength | Film-coated tablets: 20 mg/tablet (calculated as vonoprazan)

II. Physicochemical Properties

Parameter | Data (Fumarate)

Appearance | White to off-white crystalline powder

Solubility | Slightly soluble in water (approximately 0.1 mg/mL at pH 7.0), readily soluble in methanol and dimethyl sulfoxide (DMSO), soluble in ethanol

Dissociation Constant (pKa) | 4.7 (pyridine ring), 9.3 (amino group) (predicted values)

Stability | Stable for 36 months at 25℃/60% RH, store in a sealed, cool, and dry place, avoid high temperature, light, and moisture

Storage Conditions | Store at 20-25℃, short-term deviations between 15-30℃ are permitted, no refrigeration required

Chiral Characteristics | No chiral center, is a racemate, no optical isomer impurities