My360 Mycophenolic Acid Delayed Release Tablets USP 360 mg

Description:
My360 is an enteric formulation of Mycophenolate sodium that delivers the active moiety Mycophenolic acid (MPA). My360 is an immunosuppressant agent. MPA is chemically designated as(E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid sodium salt. Its empirical formula is C17H19O6 Na and molecular weight is 342.32.

Composition:

Each film-coated tablet contains enteric coated Mycophenolate Sodium 360 mg.

Mode of Action
The mechanism of action of MPA is based on interference with purine synthesis. It is a reversible, noncompetitive inhibitor of inosine monophosphate dehydrogenase (IMPDH), which is an enzyme that facilitates the conversion of inosine monophosphate (IMP) to xanthosine monophosphate, a precursor of guanine nucleotides. This blocks the de novo synthesis of guanosine nucleotides that are necessary substrates for DNA and RNA synthesis. Unlike other cell types which can use the salvage pathways, B and T lymphocytes are dependent upon the de novo pathway for the generation of guanosine. My360 is designed to reduce the adverse GI events of MPA (in particular nausea, vomiting, dyspepsia and abdominal pain).

Pharmacokinetics:
Absorption

My360 is extensively absorbed from the GI tract. The protein binding of Mycophenolic acid glucuronide (MPAG) is 82%. The free MPA concentration may increase under conditions of decreased protein binding (uremia, hepatic failure and hypoalbuminemia). Vitro studies demonstrated that the enteric-coated My360 tablet does not release MPA under acidic conditions (pH <5) as in the stomach, but is highly soluble in neutral pH conditions as in the intestine.

Distribution

Mycophenolic acid is 97% bound to plasma proteins. The mean (± SD) volume of distribution at steady state and elimination phase for MPA is 54 (± 25) L and 112 (± 48) L respectively. MPA is highly protein bound to albumin >98%. The protein binding of Mycophenolic acid glucuronide (MPAG) is 82%. The free MPA concentration may increase under conditions of decreased protein binding (uremia, hepatic failure, and hypoalbuminemia).

Metabolism

Mycophenolate is converted to active MPA, which undergoes enterohepatic recirculation. MPA is metabolised by glucuronidation to the inactive glucuronide.

Excretion

Via urine (as the glucuronide and negligible amounts of MPA); via faeces (about 6% of a dose). Mean half-life of MPA: 17.9 hours (as oral Mycophenolate mofetil) and 16.6 hours (as IV Mycophenolate mofetil); 12 hours (as Mycophenolate sodium).

Indication

Mycophenolate Sodium is indicated for the prophylaxis of organ rejection in patients receiving allogenic renal transplants, administered in combination with Cyclosporine and corticosteroids.

Contraindication

My360 is contraindicated in patients with a hypersensitivity to Mycophenolic acid, Mycophenolate mofetil (MMF) or to any of its excipients.

Precautions

Monitoring: Perform complete blood counts weekly during first month of treatment, twice monthly for second and third months, then monthly throughout the first year.

GI hemorrhage: Since Mycophenolate has been associated with an increased incidence of GI adverse events, including infrequent cases of GI tract ulceration, hemorrhage and perforation.

Delayed renal graft function post transplant: No dose adjustment is recommended for these patients.