Saxagliptin

Synonyms: (1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.0^3,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, BMS-477118, Onglyza, Komboglyze

Saxagliptin is a potent, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor developed for the treatment of type 2 diabetes. It is a synthetic small molecule that belongs to the gliptin class and is characterized by a nitrile-pyrrolidine scaffold. Unlike some other DPP-4 inhibitors, saxagliptin is rapidly absorbed and exhibits a unique metabolic profile, forming an active metabolite (5-hydroxy saxagliptin) that retains significant inhibitory activity.

Chemically, saxagliptin is a cyclopropyl-fused pyrrolidine-carbonitrile derivative. Its structure includes a 3-hydroxyadamantyl group, which contributes to its high selectivity and prolonged duration of action. The compound is typically manufactured as the free base or as the hydrochloride salt, with the free base being the most common form for pharmaceutical formulations.

In the pharmaceutical industry, saxagliptin is primarily used as an active pharmaceutical ingredient (API) in the production of oral antidiabetic medications. It is often combined with metformin or other antidiabetic agents to improve glycemic control in patients with type 2 diabetes. The API is subject to stringent quality control measures to ensure high purity and consistent performance.

Function & Mechanism

• DPP-4 inhibition: Saxagliptin binds to the active site of DPP-4, preventing the degradation of incretin hormones such as GLP-1 and GIP.
• Incretin enhancement: By inhibiting DPP-4, saxagliptin increases the levels of active incretins, leading to enhanced insulin secretion and reduced glucagon release in a glucose-dependent manner.
• Glycemic control: The net effect is improved postprandial and fasting glucose control, with a low risk of hypoglycemia when used as monotherapy.
• Selectivity: Saxagliptin is highly selective for DPP-4 over other related enzymes such as DPP-8 and DPP-9, minimizing potential off-target effects.
• Active metabolite: The major metabolite, 5-hydroxy saxagliptin, also inhibits DPP-4, contributing to the overall pharmacological effect.

Source & Standardization

• Source: Synthetic chemical synthesis
• Manufacturing process: Multi-step organic synthesis starting from chiral building blocks, followed by purification and crystallization.
• Standardization: ≥99.0% (HPLC), with strict control of impurities and residual solvents.
• Forms: White to off-white crystalline powder; also available as hydrochloride salt upon request.
• Applications: API for oral solid dosage forms (tablets), used in combination with metformin or other antidiabetic agents.

Quality Specifications (QC Tests)

Bulk Supply & Documentation

• Monthly capacity: 500 kg
• Lead time: 3-5 business days (stock items)
• Documentation: COA, MSDS, TDS, and regulatory support available upon request
• Packaging: 25 kg fiber drum with double polyethylene liners, or as per customer requirements

Frequently Asked Questions

What is the minimum order quantity (MOQ) for Saxagliptin?

Our standard MOQ is 1 kg. For smaller quantities, please contact our sales team to discuss your specific needs.

Do you provide a Certificate of Analysis (COA) and samples?

Yes, a COA is provided with every shipment. Samples are available upon request to qualified customers for evaluation purposes.

What is the typical lead time for bulk orders?

Lead time is generally 3-5 business days after order confirmation, depending on the quantity and current production schedule.

Contact & Ordering Information

• Company: LyvBio Co., Ltd.
• Address: Room 5-0203, Courtyard 205, Lianhu District, Xi’an, Shaanxi, China
• Email: info@lyvbio.com
• Phone: +86-29-65816888

Learn more about our quality control and certifications, or send us your specification for a quotation.