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Dagliflozin monohydrate

1032613-10-5 (anhydrous: 461432-26-8)

\(C_{21}H_{25}ClO_6\cdot H_2O\) (anhydrous: \(C_{21}H_{25}ClO_6\))

410.88 (anhydrous: 392.87)

Dagliflozin has a structure composed of a tricyclic core with a chlorine atom, an ether – linked sugar – like moiety, and other functional groups. In the monohydrate form, there is one molecule of water associated with the anhydrous structure. The overall structure enables it to interact with the sodium – glucose co – transporter 2 (SGLT2) in the body.

Usually appears as a white to off – white crystalline powder.

Sparingly soluble in water. Solubility is enhanced in organic solvents like ethanol and DMSO. This solubility profile is important in the development of pharmaceutical formulations, such as tablets, capsules, or oral suspensions.

SGLT2 inhibitor

Similar to other SGLT2 inhibitors, dagliflozin monohydrate inhibits the SGLT2 in the proximal renal tubules. By blocking this transporter, it reduces the reabsorption of glucose from the glomerular filtrate back into the bloodstream. As a result, more glucose is excreted in the urine, leading to a decrease in blood glucose levels without the need for insulin secretion.

Type 2 Diabetes Mellitus: Approved for the treatment of type 2 diabetes. It can be used as monotherapy or in combination with other antidiabetic drugs such as metformin, sulfonylureas, or insulin. Dagliflozin monohydrate helps to control blood sugar levels and may also contribute to improvements in HbA1c levels, as well as body weight management due to the caloric loss from glucose excretion in the urine.

Generally stable under normal storage conditions, typically at room temperature and in a dry environment. However, exposure to high humidity, extreme temperatures, or prolonged exposure to light can cause degradation, potentially reducing its potency over time.

Common side effects include genital mycotic infections, urinary tract infections, polyuria, and thirst, which are similar to those of other SGLT2 inhibitors. There is also a risk of euglycemic diabetic ketoacidosis, although it is rare. Additionally, it may increase the risk of orthostatic hypotension, especially in patients who are volume – depleted or taking medications that can cause fluid loss, such as diuretics. Some studies have also associated SGLT2 inhibitors with an increased risk of bone fractures, but the evidence is still being evaluated.