Introduction: The Post-Patent Opportunity

With the patent protection for Forxiga (Farxiga) expiring in major markets, Dapagliflozin has become one of the most sought-after molecules in the generic pharmaceutical industry. As an SGLT2 inhibitor used for diabetes, heart failure, and chronic kidney disease, the market potential is vast. However, sourcing Dapagliflozin API requires a deep understanding of its chemical forms and stability profiles.

The Critical Distinction: Propanediol vs. Amorphous

Buyers must be precise when requesting quotes. Dapagliflozin is commonly available in two primary forms:

1. Dapagliflozin Propanediol Monohydrate (CAS 960404-48-2): This is the solvated form used in many originator formulations. It offers superior stability against hygroscopicity compared to the base form.

2. Dapagliflozin Amorphous (CAS 461432-26-8): While the CAS 461432-26-8 refers to the base molecule, the amorphous form is often used by generic companies to design alternative formulations.

Sourcing the wrong form can lead to patent infringement or stability failures during stability testing (accelerated conditions).

Quality Attributes and Synthesis

The synthesis of Dapagliflozin involves complex C-glycosylation steps. A key quality indicator is the control of the intermediate 5-Bromo-2-chloro-4'-ethoxydiphenylmethane.

• Residual Solvents: Since the propanediol form involves a solvate, the stoichiometry of propanediol to the active ingredient must be precise (typically 1:1).

• Moisture Content: For the amorphous form, moisture control is critical as it is highly hygroscopic.

• Purity: High Purity Dapagliflozin (99%+) is the standard, but specific attention must be paid to the alpha-anomer impurity, which should be strictly limited.

Finding the Right Dapagliflozin Supplier

When evaluating a Dapagliflozin API Supplier, consider the following checklist:

• Capacity: Can they support commercial scale (metric tons) or only R&D quantities?

• Regulatory Status: Is the site USFDA approved or GMP certified?

• Cost Efficiency: With the price per kg dropping due to generic competition, does the supplier have cost advantages through efficient synthesis routes?

Summary

Dapagliflozin represents a cornerstone for modern metabolic portfolios. By securing a high-quality, stable source of Dapagliflozin Propanediol Monohydrate or the Amorphous form, pharmaceutical companies can ensure a successful product launch in the competitive generic market.