Mycamine - General Information
Mycamine is an antifungal drug. It belongs to the antifungal class of compounds known as echinocandins and exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall.
Pharmacology of Mycamine
Formerly known as FK463, micafungin is a novel antifungal agent. It is a glucan synthesis inhibitor of the echinocandin structural class. The U.S. Food and Drug Administration approved micafungin in March 2005. Mycamine inhibits an enzyme essential for fungal cell-wall synthesis and is fungicidal (lethal) for Candida. Mycamine can be used concomitantly with a variety of other drugs, including the HIV protease inhibitor ritonavir and the transplant medications cyclosporine and tacrolimus.
Mycamine for patients
A total of 11 clinical drug-drug interaction studies were conducted in healthy volunteers to evaluate the potential for interaction between MYCAMINE and mycophenolate mofetil, cyclosporine, tacrolimus, prednisolone, sirolimus, nifedipine, fluconazole, ritonavir, and rifampin. In these studies, no interaction that altered the pharmacokinetics of micafungin was observed.
There was no effect of a single dose or multiple doses of MYCAMINE on mycophenolate mofetil, cyclosporine, tacrolimus, prednisolone, and fluconazole pharmacokinetics.
Sirolimus AUC was increased by 21% with no effect on Cmax in the presence of steady-state MYCAMINE compared with sirolimus alone. Nifedipine AUC and Cmax were increased by 18% and 42%, respectively, in the presence of steady-state MYCAMINE compared with nifedipine alone. Patients receiving sirolimus or nifedipine in combination with MYCAMINE should be monitored for sirolimus or nifedipine toxicity and sirolimus or nifedipine dosage should be reduced if necessary.
Micafungin is not an inhibitor of P-glycoprotein and, therefore, would not be expected to alter P-glycoprotein-mediated drug transport activity.
MYCAMINE is contraindicated in patients with hypersensitivity to any component of this product.
Additional information about Mycamine
Mycamine Indication: For use in the treatment of patients with esophageal candidiasis and prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplantation.
Mechanism Of Action: Mycamine inhibits the synthesis of 1,3-b-D-glucan, an essential component of fungal cell walls, which is not present in mammalian cells.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Micafungin
Synonyms: Not Available
Drug Category: Antifungals
Drug Type: Small Molecule; Approved
Absorption: Not Available
Toxicity (Overdose): Intravenous LD50 in rats is 125mg/kg. In dogs it is >200mg/kg. No cases of overdosage have been reported. Repeated daily doses up to 8 mg/kg (maximum total dose of 896 mg) in adult patients have been administered in clinical trials with no reported dose-limiting toxicity. The minimum lethal dose is 125 mg/kg in rats, equivalent to 8.1 times the recommended human clinical dose for esophageal candidiasis based on body surface area comparisons.
Protein Binding: Highly (>99%) protein bound in vitro, independent of plasma concentrations over the range of 10 to 100 µg/mL. The primary binding protein is albumin; however, micafungin, at therapeutically relevant concentrations, does not competitively displace bilirubin binding to albumin. Micafungin also binds to a lesser extent to a1-acid-glycoprotein.
Biotransformation: Micafungin is metabolized to M-1 (catechol form) by arylsulfatase, with further metabolism to M-2 (methoxy form) by catechol-O-methyltransferase. M-5 is formed by hydroxylation at the side chain (w-1 position) of micafungin catalyzed by cytochrome P450 (CYP) isozymes. Even though micafungin is a substrate for and a weak inhibitor of CYP3A in vitro, hydroxylation by CYP3A is not a major pathway for micafungin metabolism in vivo.
Half Life: 14-17 hours
Dosage Forms of Mycamine: Injection, powder, lyophilized, for solution Intravenous drip
Chemical IUPAC Name: Not Available
Chemical Formula: C56H71N9O23S
Micafungin on Wikipedia: https://en.wikipedia.org/wiki/Micafungin
Organisms Affected: Aspergillis, Candida and other fungi