Peringatan Keamanan

Side effects include those of other statins, such as myalgias, abdominal pain, nausea. It also has a higher chance of giving more severe side effects related to myotoxicity (myopathy, myositis, rhabdomyolysis), and hepatotoxicity, than other statins. Due to these major side effects and their enhanced rate of occurance, Mevastatin is not given therapeutically.

Mevastatin

DB06693

small molecule experimental

Deskripsi

Mevastatin or compactin is a cholesterol-lowering agent isolated from Penicillium citinium. It was the first discovered agent belonging to the class of cholesterol-lowering medications known as statins. During a search for antibiotic compounds produced by fungi in 1971, Akira Endo at Sankyo Co. (Japan) discovered a class of compounds that appeared to lower plasma cholesterol levels. Two years later, the research group isolated a compound structurally similar to hydroxymethylglutarate (HMG) that inhibited the incorporation of acetate. The compound was proposed to bind to the reductase enzyme and was named compactin. Mevastatin is a competitive inhibitor of HMG-Coenzyme A (HMG-CoA) reductase with a binding affinity 10,000 times greater than the HMG-CoA substrate itself. Mevastatin is a pro-drug that is activated by in vivo hydrolysis of the lactone ring. It has served as one of the lead compounds for the development of the synthetic compounds used today.

Struktur Molekul 2D

Berat 390.52
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Avoid grapefruit products.

Interaksi Obat

126 Data
Acipimox Acipimox may increase the myopathic rhabdomyolysis activities of Mevastatin.
Bezafibrate Bezafibrate may increase the myopathic rhabdomyolysis activities of Mevastatin.
Ciprofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ciprofibrate is combined with Mevastatin.
Colchicine Colchicine may increase the myopathic rhabdomyolysis activities of Mevastatin.
Daptomycin The risk or severity of myopathy can be increased when Mevastatin is combined with Daptomycin.
Gemfibrozil The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Mevastatin.
Niacin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Mevastatin.
Pazopanib Mevastatin may increase the hepatotoxic activities of Pazopanib.
Raltegravir The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Mevastatin.
Trabectedin The risk or severity of myopathy and rhabdomyolysis can be increased when Mevastatin is combined with Trabectedin.
Amiodarone The metabolism of Mevastatin can be increased when combined with Amiodarone.
Danazol The serum concentration of Mevastatin can be increased when it is combined with Danazol.
Colestipol Colestipol can cause a decrease in the absorption of Mevastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Mevastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Mevastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Mevastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fusidic acid The risk or severity of rhabdomyolysis can be increased when Fusidic acid is combined with Mevastatin.
Clofibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Clofibrate is combined with Mevastatin.
Fenofibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Fenofibrate is combined with Mevastatin.
Etofibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Etofibrate is combined with Mevastatin.
Simfibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Simfibrate is combined with Mevastatin.
Ronifibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Ronifibrate is combined with Mevastatin.
Aluminium clofibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Aluminium clofibrate is combined with Mevastatin.
Clofibride The risk or severity of myopathy and rhabdomyolysis can be increased when Clofibride is combined with Mevastatin.
Fenofibric acid The risk or severity of myopathy and rhabdomyolysis can be increased when Fenofibric acid is combined with Mevastatin.
Lanthanum carbonate The absorption of Mevastatin can be decreased when combined with Lanthanum carbonate.
Clarithromycin The metabolism of Mevastatin can be decreased when combined with Clarithromycin.
Ubidecarenone The risk or severity of myopathy and rhabdomyolysis can be decreased when Ubidecarenone is combined with Mevastatin.
Erlotinib The metabolism of Mevastatin can be decreased when combined with Erlotinib.
Leuprolide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Leuprolide is combined with Mevastatin.
Somatotropin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Somatotropin is combined with Mevastatin.
Infliximab The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Infliximab is combined with Mevastatin.
Cyclosporine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cyclosporine is combined with Mevastatin.
Pravastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pravastatin is combined with Mevastatin.
Baclofen The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Baclofen is combined with Mevastatin.
Sildenafil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Sildenafil is combined with Mevastatin.
Indinavir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Indinavir is combined with Mevastatin.
Lovastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Lovastatin is combined with Mevastatin.
Cladribine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cladribine is combined with Mevastatin.
Phenytoin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Phenytoin is combined with Mevastatin.
Pamidronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pamidronic acid is combined with Mevastatin.
Mefloquine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Mefloquine is combined with Mevastatin.
Tacrine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Tacrine is combined with Mevastatin.
Carbimazole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Carbimazole is combined with Mevastatin.
Cerivastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cerivastatin is combined with Mevastatin.
Trimethoprim The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Trimethoprim is combined with Mevastatin.
Betamethasone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Betamethasone is combined with Mevastatin.
Montelukast The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Montelukast is combined with Mevastatin.
Zidovudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Zidovudine is combined with Mevastatin.
Cimetidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cimetidine is combined with Mevastatin.
Ritonavir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ritonavir is combined with Mevastatin.
Lercanidipine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Lercanidipine is combined with Mevastatin.
Ciprofloxacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ciprofloxacin is combined with Mevastatin.
Vincristine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Vincristine is combined with Mevastatin.
Propylthiouracil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Propylthiouracil is combined with Mevastatin.
Methotrexate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Methotrexate is combined with Mevastatin.
Enalapril The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Enalapril is combined with Mevastatin.
Nizatidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nizatidine is combined with Mevastatin.
Ivermectin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ivermectin is combined with Mevastatin.
Chloroquine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Chloroquine is combined with Mevastatin.
Triamcinolone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Triamcinolone is combined with Mevastatin.
Alendronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Alendronic acid is combined with Mevastatin.
Simvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Simvastatin is combined with Mevastatin.
Stavudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Stavudine is combined with Mevastatin.
Nafarelin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Nafarelin is combined with Mevastatin.
Amphotericin B The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Amphotericin B is combined with Mevastatin.
Mycophenolate mofetil The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Mycophenolate mofetil is combined with Mevastatin.
Lamivudine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Lamivudine is combined with Mevastatin.
Ibandronate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ibandronate is combined with Mevastatin.
Propofol The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Propofol is combined with Mevastatin.
Terbinafine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Terbinafine is combined with Mevastatin.
Penicillamine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Penicillamine is combined with Mevastatin.
Ranitidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ranitidine is combined with Mevastatin.
Tacrolimus The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Tacrolimus is combined with Mevastatin.
Eprosartan The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Eprosartan is combined with Mevastatin.
Risedronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Risedronic acid is combined with Mevastatin.
Bumetanide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Bumetanide is combined with Mevastatin.
Triazolam The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Triazolam is combined with Mevastatin.
Ethanol The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ethanol is combined with Mevastatin.
Salmeterol The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Salmeterol is combined with Mevastatin.
Isoniazid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Isoniazid is combined with Mevastatin.
Methyldopa The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Methyldopa is combined with Mevastatin.
Isotretinoin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Isotretinoin is combined with Mevastatin.
Cytarabine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cytarabine is combined with Mevastatin.
Ganciclovir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ganciclovir is combined with Mevastatin.
Letrozole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Letrozole is combined with Mevastatin.
Sulfamethoxazole The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Sulfamethoxazole is combined with Mevastatin.
Minocycline The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Minocycline is combined with Mevastatin.
Procainamide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Procainamide is combined with Mevastatin.
Norfloxacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Norfloxacin is combined with Mevastatin.
Atorvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Atorvastatin is combined with Mevastatin.
Fluvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Fluvastatin is combined with Mevastatin.
Rosuvastatin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Rosuvastatin is combined with Mevastatin.
Ofloxacin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ofloxacin is combined with Mevastatin.
Procarbazine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Procarbazine is combined with Mevastatin.
Captopril The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Captopril is combined with Mevastatin.
Paclitaxel The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Paclitaxel is combined with Mevastatin.
Saquinavir The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Saquinavir is combined with Mevastatin.
Metoclopramide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Metoclopramide is combined with Mevastatin.
Dexamethasone The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Dexamethasone is combined with Mevastatin.

Target Protein

3-hydroxy-3-methylglutaryl-coenzyme A reductase HMGCR

Referensi & Sumber

Synthesis reference: Scott Primrose, David King, Ed Yaworski, Jayaramaiyer Radhakrishnan, David He, Xinfa Xiao, "Fermentation process for preparation of compactin." U.S. Patent US5691173, issued September, 1977.

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Sekuens Gen/Protein (FASTA)

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