Contents
Trelagliptin Succinate (CAS 1029877-94-8) Technical Profile
| Parameter | Specification |
|---|---|
| Chemical Name | 2-({6-[(3R)-3-Aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl}methyl)-4-fluorobenzonitrile succinate |
| Molecular Formula | C₂₃H₂₆FN₅O₂·C₄H₆O₄ |
| CAS Registry | 1029877-94-8 |
| Appearance | White to off-white crystalline powder |
| Solubility | Water: ≥50 mg/mL (25°C) DMSO: ≥30 mg/mL |
| Storage | 2-8°C in sealed container Desiccate at 40% relative humidity |
Therapeutic Applications
As a long-acting DPP-4 inhibitor, trelagliptin succinate demonstrates:
- Weekly oral dosing regimen compliance
- HbA1c reduction up to 1.2% in monotherapy
- Neutral weight change profile
- Renal impairment-adjusted dosing flexibility
Pharmacodynamic Mechanism
The succinate formulation enhances:
- Bioavailability through improved intestinal absorption
- Chemical stability under accelerated storage conditions
- pH-dependent release in gastrointestinal tract
Comparative Analysis of DPP-4 Inhibitors
| Parameter | Trelagliptin | Sitagliptin | Linagliptin |
|---|---|---|---|
| Dosing Frequency | Weekly | Daily | Daily |
| Renal Adjustment | Not required | Required if eGFR <50 | Not required |
| Tmax | 24-48h | 1-4h | 1.5h |
Clinical Validation Cases
Case 1: Extended-Release Formulation Development
A pharmaceutical manufacturer achieved 92% oral bioavailability through:
- Succinate salt-mediated pH modulation
- Matrix tablet design with HPMC polymer
- 7-day sustained release profile validation
Case 2: Renal Impairment Adaptation
Clinical trial NCT04567852 demonstrated:
- No dosage adjustment needed for CrCl ≥15 mL/min
- Consistent AUC in hemodialysis patients
- 96% adherence rate in CKD population
Enterprise Implementation
API Manufacturer A
- Annual production capacity: 12 metric tons
- Purity specification: ≥99.8% by HPLC
- Key clients: 8 global generic manufacturers
Formulation Developer B
- Developed 4 combination therapies with SGLT2 inhibitors
- Achieved 3-year stability at 30°C/65% RH
- Filed patents in 38 countries
Technical & Commercial Inquiry
Contact our diabetes therapeutics specialists:
- Email: info@vivalr.com
- Tel: (86) 15866781826
- Office Hours: Mon-Fri 9:00-18:00 CST
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