Trelagliptin Succinate

Indications

Trelagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It is a highly selective dipeptidyl peptidase-4 inhibitor that is typically used as an add on treatment when the first line treatment of metformin is not achieving the expected glycemic goals; though it has been approved for use as a first line treatment when metformin cannot be used.

Pharmacology

It controls blood glucose levels by selectively and continually inhibiting DPP-4, an enzyme that causes the inactivation of glucagon-like peptide-1 and glucagon-dependent insulinotropic polypeptide, incretin hormones that play an important role in blood glucose regulation. The inhibition of DPP-4 increases insulin secretion depending on blood glucose concentration, thereby controlling blood glucose levels. It is indicated for the treatment of type 2 diabetes.

Dosage & Administration

100 mg of Trelagliptin is administered to adults once weekly by mouth. This has lesser hypoglycemic events and 4 and 12-fold more potent than Alogliptin and Sitagliptin.

Contraindications

Study subjects meeting any of the following criteria will not be included in this study:
  • Patients under treatment with trelagliptin for type 2 diabetes at the start of screening.
  • Patients with a diagnosis of type 1 diabetes.
  • Patients with severe renal impairment or renal failure (e.g., eGFR < 30 mL/min/1.73 m2 or on dialysis).
  • Patients with serious heart disease or a cerebrovascular disorder, or a serious pancreatic, blood, or other disease.
  • Patients with a history of gastrointestinal resection.
  • Patients with a proliferative diabetic retinopathy.
  • Patients with malignancy.
  • Patients with a history of hypersensitivity or allergy to DPP-4 inhibitors.
  • Patients who are pregnant, breast-feeding, possibly pregnant, or planning to become pregnant.
  • Patients who may need to add or discontinue concomitant medication or change the dose during the study period.
  • Patients who will require treatment with a prohibited concomitant medication during the study period.
  • Patients participating in other clinical studies.
  • Patients assessed as ineligible for any other reason by the investigators.

Side Effects

Among 901 domestic clinical trial cases up to the time of approval, 103 cases ( 11.4%) showed clinical results that included abnormalities and side effects. These mainly included hypoglycemia, nasopharyngitis, and elevated lipase.

Given the appearance of serious side effects such as hypoglycemia (0.1~5%) , administer medication in conjunction with close observation of patient status. Other DPP-4 inhibitors have been reported to present serious hypoglycemia in combination with Sulfonylurea medications as well as some cases of loss of consciousness. Moreover, decreased blood sugar from the use of this medication, once confirmed, can be remedied by giving sucrose. However, hypoglycemia resulting from a combination with glucosidase inhibitors should be treated with fructose.

Pregnancy & Lactation

No study has performed in patients who are pregnant, breast-feeding, possibly pregnant, or planning to become pregnant.

Precautions & Warnings

(provide cautious dosage to the following patients): The following patients or circumstances
  • Patients with moderate kidney function disorder
  • Patients undergoing treatment with sulfonylurea drugs or insulin medication [there are reports of severe hypotension with use in combination with other DPP-4 inhibitors]
  • Hypopituitarism or hypoadrenalism
  • Malnutrition, starvation, irregular eating patterns, insufficient eating, or hyposthenia
  • Vigorous exercise
  • Patients who consume excessive alcohol

Therapeutic Class

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

Storage Conditions

Store at 25°C; excursions permitted to 15°-30°C. Dispense medication in the original container to protect from exposure to high humidity and light. Keep out of the reach of children