Forxiga
[CAS# 960404-48-2]

Identification

• Classification: API >> Circulatory system medication
• Name: Forxiga
• Synonyms: Dapagliflozin propylene glycolate hydrate
• Molecular Formula: C₂₁H₂₅ClO₆.C₃H₈O₂.H₂O
• Molecular Weight: 502.98
• CAS Registry Number: 960404-48-2
• EC Number: 811-335-4
• SMILES: CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)Cl.C[C@@H](CO)O.O

Properties

• Solubility: DMSO 10 mM (Expl.)

Safety Data

• Hazard Symbols: GHS07 Warning
• Risk Statements: H302-H315-H319-H335
• Safety Statements: P261-P305+P351+P338

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Acute toxicity	Acute Tox.	4	H302
Reproductive toxicity	Lact.	-	H362
Eye irritation	Eye Irrit.	2	H319
Specific target organ toxicity - repeated exposure	STOT RE	1	H372
Reproductive toxicity	Repr.	1B	H360
Reproductive toxicity	Repr.	1B	H360D
Reproductive toxicity	Repr.	2	H361d
Chronic hazardous to the aquatic environment	Aquatic Chronic	2	H411
Reproductive toxicity	Repr.	2	H361
Specific target organ toxicity - repeated exposure	STOT RE	2	H373

Discovery and Applications

Forxiga is the brand name for the drug dapagliflozin, a pharmaceutical compound classified as a sodium-glucose co-transporter 2 (SGLT2) inhibitor. It was developed and approved in the early 2010s for the treatment of type 2 diabetes mellitus, and subsequently for other indications related to cardiovascular and renal health.

Dapagliflozin works by selectively inhibiting the SGLT2 protein in the proximal tubules of the kidneys. SGLT2 is responsible for reabsorbing the majority of glucose filtered by the kidneys back into the bloodstream. By blocking this transporter, dapagliflozin reduces glucose reabsorption, leading to increased urinary glucose excretion. This mechanism lowers blood glucose levels independently of insulin secretion or action.

Clinically, dapagliflozin is prescribed primarily for improving glycemic control in adults with type 2 diabetes, often in combination with other antidiabetic agents. Beyond its glucose-lowering effects, dapagliflozin has demonstrated benefits in reducing the risk of hospitalization for heart failure and in slowing the progression of chronic kidney disease in patients with or without diabetes.

Dapagliflozin is administered orally, typically once daily. It has good bioavailability and is metabolized mainly via the liver enzyme UGT1A9 to inactive metabolites, which are excreted primarily through the urine and feces. The elimination half-life is approximately 12 to 13 hours, supporting once-daily dosing.

Adverse effects of dapagliflozin can include urinary tract infections, genital infections, and increased urination due to osmotic diuresis caused by glucosuria. Rare but serious risks include ketoacidosis and volume depletion. Patient monitoring and appropriate clinical management are important to minimize these risks.

Forxiga has become a significant therapeutic option not only for diabetes management but also for patients with heart failure and chronic kidney disease, reflecting its multifaceted clinical benefits beyond glycemic control.

In summary, Forxiga (dapagliflozin) is an SGLT2 inhibitor used mainly to treat type 2 diabetes by promoting urinary glucose excretion. Its mechanism contributes to blood sugar reduction and additional cardiovascular and renal benefits, with a well-established safety and efficacy profile in clinical practice.

References

2009. A study of dapagliflozin in patients with type 2 diabetes receiving high doses of insulin plus insulin sensitizers: applicability of a novel insulin-independent treatment. Diabetes Care, 32(9).
DOI: 10.2337/dc09-0517

2018. Efficacy and Safety of Dapagliflozin in Patients With Inadequately Controlled Type 1 Diabetes: The DEPICT-1 52-Week Study. Diabetes Care, 41(12).
DOI: 10.2337/dc18-1087

2024. Comparison of safety profiles for dapagliflozin based on EMA and FDA safety issues: Challenges and future of post-marketing surveillance in Korea. PLOS ONE, 19(11).
DOI: 10.1371/journal.pone.0314363