XELEVIA

What it is

XELEVIA is available for oral use as film coated tablets containing sitagliptin phosphate monohydrate equivalent to 25, 50 or 100 mg of free base. Sitagliptin is a member of a class of oral anti-hyperglycaemic agents called dipeptidyl peptidase 4 (DPP-4) inhibitors, which improve glycaemic control in patients with type 2 diabetes by enhancing the levels of active incretin hormones.

Approved indications

— Adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus as monotherapy when metformin is considered inappropriate due to intolerance. — Adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes mellitus in combination with other anti-hyperglycaemic agents, including insulin.

Dosing overview

The recommended dose of XELEVIA is 100 mg once daily as monotherapy, or as combination therapy with metformin, or a sulfonylurea, insulin (with or without metformin), a thiazolidinedione, or combination therapy with metformin and a sulfonylurea. For patients with renal impairment, dosing is adjusted by estimated glomerular filtration rate (eGFR). For patients with eGFR ≥ 45 mL/min/1.73 m² to < 90 mL/min/1.73 m², no dosage adjustment for XELEVIA is required. For patients with eGFR ≥ 30 mL/min/1.73 m² to < 45 mL/min/1.73 m², the dose of XELEVIA is 50 mg once daily. For patients with eGFR ≥ 15 mL/min/1.73 m² to < 30 mL/min/1.73 m² or with end-stage renal disease (eGFR < 15 mL/min/1.73 m²), including those requiring haemodialysis or peritoneal dialysis, the dose of XELEVIA is 25 mg once daily.

Key safety warnings

**Pancreatitis.** There have been reports of acute pancreatitis, including fatal and non-fatal haemorrhagic or necrotising pancreatitis, in patients taking sitagliptin. Patients should be informed of the characteristic symptom of acute pancreatitis: persistent, severe abdominal pain. If pancreatitis is suspected, XELEVIA and other potentially suspect medicinal products should be discontinued. **Hypersensitivity reactions.** There have been postmarketing reports of serious hypersensitivity reactions in patients treated with XELEVIA. These reactions include anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome. Onset of these reactions occurred within the first 3 months after initiation of treatment with XELEVIA, with some reports occurring after the first dose. **Arthralgia.** There have been post-marketing reports of joint pain, which may be severe, in patients taking DPP-4 inhibitors. Onset of symptoms following initiation of treatment may be rapid or may occur after longer periods. **Bullous pemphigoid.** Postmarketing cases of bullous pemphigoid requiring hospitalisation have been reported with DPP-4 inhibitor use. Tell patients to report development of blisters or erosions while receiving XELEVIA. If bullous pemphigoid is suspected, XELEVIA should be discontinued and referral to a dermatologist should be considered for diagnosis and appropriate treatment. **Hypoglycaemia with sulfonylureas or insulin.** Hypoglycaemia has been observed when XELEVIA was used in combination with insulin or a sulfonylurea. When XELEVIA is used in combination with a sulfonylurea or with insulin, reduction in the dose of sulfonylurea or insulin may be considered to reduce the risk of sulfonylurea- or insulin-induced hypoglycaemia.

Contraindications

XELEVIA is contraindicated in patients who are hypersensitive to any components of this product. XELEVIA should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.

PBS listing

XELEVIA is available in three strengths: 25 mg, 50 mg, and 100 mg film-coated tablets, with ARTG registrations first listed on 2 August 2023. Information regarding PBS listing status, restriction type, and ex-manufacturer pricing is not available in the provided source documents.

Regulatory history

XELEVIA sitagliptin (as phosphate monohydrate) in strengths of 25 mg, 50 mg, and 100 mg film-coated tablets was first listed on the Australian Register of Therapeutic Goods on 2 August 2023 under licence category RE (sponsor: Merck Sharp & Dohme).