Peringatan Keamanan

The LD50 of oritavancin in rats is >500m mg/kg.L12870 Prescribing information indicates no experience with overdose during the clinical program for oritavancin, however, an overdose is likely to result in an increased risk of adverse effects, such as headache, nausea vomiting, and diarrhea. This drug is not dialyzable, and in the case of an overdose, supportive measures should be undertaken.L8492

Oritavancin

DB04911

small molecule approved investigational

Deskripsi

Oritavancin is a glycopeptide antibiotic used for the treatment of skin infections. It was developed by The Medicines Company (acquired by Novartis).L12858 Oritavancin was initially approved by the FDA in 2014 and formulated to combat susceptible gram-positive bacteria that cause skin and skin structure infections. It boasts the option of single-dose administration and has been proven as non-inferior to a full course of vancomycin therapy.A39384,A193482,L8492

On March 12, 2021 the FDA approved Kimyrsa, a complete course of therapy in a single, 1 hour 1200 mg infusion.L32634 Orbactiv, the other FDA approved oritavancin product, is administered over a 3 hour infusion and contains a lower dose of 400 mg. Marketed by Melinta Therapeutics, Kimyrsa offers effective and time-efficient treatment for skin and skin structure infections.L32629

Struktur Molekul 2D

Berat 1793.101
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average terminal half-life of oritavancin is about 245 hours.[L8492] A pharmacokinetic study revealed a terminal half-life ranging from 135.8-273.8 hours.[A2933]
Volume Distribusi The volume of distribution of oritavancin is estimated at 87.6 L, suggesting extensive tissue distribution.[L8492]
Klirens (Clearance) The clearance of oritavancin is approximately 0.445 L/h.[L8492] One study revealed a renal clearance of 0.457 mL/min.[A2933]

Absorpsi

Pharmacokinetic analysis of oritavancin revealed a Cmax of 138 and ?g/mL and an AUC0-? of 2800 ?g•h/mL.L8492 The AUC0-t in a study of healthy volunteers after an 800 mg dose 1,1111 ?g•h/mL.A2932 was also be Another pharmacokinetic study reported a Cmax of 4.7-7.6 micrograms/mL, generally achieved within 24 hours of administration.A2933

Metabolisme

In vitro studies on human hepatocytes suggest that oritavancin is not metabolized, and is excreted unchanged.A185297,L8492

Rute Eliminasi

Oritavancin is excreted as unchanged drug in both the urine and feces. Less than 5% has been recovered in the urine, and 1% has been recovered in the feces.A2933,L8492

Interaksi Obat

636 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Oritavancin.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Oritavancin.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Oritavancin.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Oritavancin.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Oritavancin.
Perampanel The metabolism of Perampanel can be increased when combined with Oritavancin.
Ardeparin The therapeutic efficacy of Ardeparin can be decreased when used in combination with Oritavancin.
Heparin The therapeutic efficacy of Heparin can be decreased when used in combination with Oritavancin.
Enoxaparin The therapeutic efficacy of Enoxaparin can be decreased when used in combination with Oritavancin.
Sulodexide The therapeutic efficacy of Sulodexide can be decreased when used in combination with Oritavancin.
Semuloparin The therapeutic efficacy of Semuloparin can be decreased when used in combination with Oritavancin.
Danaparoid The therapeutic efficacy of Danaparoid can be decreased when used in combination with Oritavancin.
Dalteparin The therapeutic efficacy of Dalteparin can be decreased when used in combination with Oritavancin.
Tinzaparin The therapeutic efficacy of Tinzaparin can be decreased when used in combination with Oritavancin.
Nadroparin The therapeutic efficacy of Nadroparin can be decreased when used in combination with Oritavancin.
Bemiparin The therapeutic efficacy of Bemiparin can be decreased when used in combination with Oritavancin.
Parnaparin The therapeutic efficacy of Parnaparin can be decreased when used in combination with Oritavancin.
Reviparin The therapeutic efficacy of Reviparin can be decreased when used in combination with Oritavancin.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Oritavancin.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Oritavancin.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Oritavancin.
Segesterone acetate The metabolism of Segesterone acetate can be increased when combined with Oritavancin.
Diethylstilbestrol The metabolism of Diethylstilbestrol can be increased when combined with Oritavancin.
Etonogestrel The metabolism of Etonogestrel can be increased when combined with Oritavancin.
Desogestrel The metabolism of Desogestrel can be increased when combined with Oritavancin.
Megestrol acetate The metabolism of Megestrol acetate can be increased when combined with Oritavancin.
Levonorgestrel The metabolism of Levonorgestrel can be increased when combined with Oritavancin.
Progesterone The metabolism of Progesterone can be increased when combined with Oritavancin.
Medroxyprogesterone acetate The metabolism of Medroxyprogesterone acetate can be increased when combined with Oritavancin.
Norethisterone The metabolism of Norethisterone can be increased when combined with Oritavancin.
Estradiol The metabolism of Estradiol can be increased when combined with Oritavancin.
Ethynodiol diacetate The metabolism of Ethynodiol diacetate can be increased when combined with Oritavancin.
Mifepristone The metabolism of Mifepristone can be increased when combined with Oritavancin.
Norgestimate The metabolism of Norgestimate can be increased when combined with Oritavancin.
Ethinylestradiol The metabolism of Ethinylestradiol can be increased when combined with Oritavancin.
Mestranol The metabolism of Mestranol can be increased when combined with Oritavancin.
Drospirenone The metabolism of Drospirenone can be increased when combined with Oritavancin.
Estrone sulfate The metabolism of Estrone sulfate can be increased when combined with Oritavancin.
Octylphenoxy polyethoxyethanol The metabolism of Octylphenoxy polyethoxyethanol can be increased when combined with Oritavancin.
Cyproterone acetate The metabolism of Cyproterone acetate can be increased when combined with Oritavancin.
Trestolone The metabolism of Trestolone can be increased when combined with Oritavancin.
Norelgestromin The metabolism of Norelgestromin can be increased when combined with Oritavancin.
Gestodene The metabolism of Gestodene can be increased when combined with Oritavancin.
Hydroxyprogesterone caproate The metabolism of Hydroxyprogesterone caproate can be increased when combined with Oritavancin.
Dienogest The metabolism of Dienogest can be increased when combined with Oritavancin.
Norethynodrel The metabolism of Norethynodrel can be increased when combined with Oritavancin.
Norgestrel The metabolism of Norgestrel can be increased when combined with Oritavancin.
Cloprostenol The metabolism of Cloprostenol can be increased when combined with Oritavancin.
Gestrinone The metabolism of Gestrinone can be increased when combined with Oritavancin.
Nomegestrol The metabolism of Nomegestrol can be increased when combined with Oritavancin.
Lynestrenol The metabolism of Lynestrenol can be increased when combined with Oritavancin.
Gossypol The metabolism of Gossypol can be increased when combined with Oritavancin.
Ormeloxifene The metabolism of Ormeloxifene can be increased when combined with Oritavancin.
Chlormadinone The metabolism of Chlormadinone can be increased when combined with Oritavancin.
Norgestrienone The metabolism of Norgestrienone can be increased when combined with Oritavancin.
Quingestanol The metabolism of Quingestanol can be increased when combined with Oritavancin.
Demegestone The metabolism of Demegestone can be increased when combined with Oritavancin.
Etynodiol The metabolism of Etynodiol can be increased when combined with Oritavancin.
Testosterone enanthate The metabolism of Testosterone enanthate can be increased when combined with Oritavancin.
Estradiol benzoate The metabolism of Estradiol benzoate can be increased when combined with Oritavancin.
Estradiol cypionate The metabolism of Estradiol cypionate can be increased when combined with Oritavancin.
Estradiol valerate The metabolism of Estradiol valerate can be increased when combined with Oritavancin.
Nomegestrol acetate The metabolism of Nomegestrol acetate can be increased when combined with Oritavancin.
Norethindrone enanthate The metabolism of Norethindrone enanthate can be increased when combined with Oritavancin.
Ulipristal The metabolism of Ulipristal can be increased when combined with Oritavancin.
Phenindione The risk or severity of bleeding can be increased when Oritavancin is combined with Phenindione.
Coumarin The risk or severity of bleeding can be increased when Oritavancin is combined with Coumarin.
Tioclomarol The risk or severity of bleeding can be increased when Oritavancin is combined with Tioclomarol.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Oritavancin is combined with Ethyl biscoumacetate.
Diphenadione The risk or severity of bleeding can be increased when Oritavancin is combined with Diphenadione.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Oritavancin is combined with 4-hydroxycoumarin.
Clorindione The risk or severity of bleeding can be increased when Oritavancin is combined with Clorindione.
Azithromycin The metabolism of Azithromycin can be increased when combined with Oritavancin.
Ziprasidone The metabolism of Ziprasidone can be increased when combined with Oritavancin.
Cephalexin The metabolism of Cephalexin can be increased when combined with Oritavancin.
Fenofibrate The metabolism of Fenofibrate can be increased when combined with Oritavancin.
Atazanavir The metabolism of Atazanavir can be increased when combined with Oritavancin.
Rosuvastatin The metabolism of Rosuvastatin can be increased when combined with Oritavancin.
Allylestrenol The metabolism of Allylestrenol can be increased when combined with Oritavancin.
Roflumilast The metabolism of Roflumilast can be increased when combined with Oritavancin.
Linagliptin The metabolism of Linagliptin can be increased when combined with Oritavancin.
Vorapaxar The metabolism of Vorapaxar can be increased when combined with Oritavancin.
Suvorexant The metabolism of Suvorexant can be increased when combined with Oritavancin.
Tasimelteon The metabolism of Tasimelteon can be increased when combined with Oritavancin.
Nintedanib The metabolism of Nintedanib can be increased when combined with Oritavancin.
Tenofovir alafenamide The metabolism of Tenofovir alafenamide can be increased when combined with Oritavancin.
Dihydroergocornine The metabolism of Dihydroergocornine can be increased when combined with Oritavancin.
Duvelisib The metabolism of Duvelisib can be increased when combined with Oritavancin.
Gilteritinib The metabolism of Gilteritinib can be increased when combined with Oritavancin.
9-aminocamptothecin The metabolism of 9-aminocamptothecin can be increased when combined with Oritavancin.
Methylprednisone The metabolism of Methylprednisone can be increased when combined with Oritavancin.
Dihydroergocristine The metabolism of Dihydroergocristine can be increased when combined with Oritavancin.
Dihydroergocryptine The metabolism of Dihydroergocryptine can be increased when combined with Oritavancin.
Medical Cannabis The metabolism of Medical Cannabis can be increased when combined with Oritavancin.
Elexacaftor The metabolism of Elexacaftor can be increased when combined with Oritavancin.
Fosaprepitant The metabolism of Fosaprepitant can be increased when combined with Oritavancin.
Lefamulin The metabolism of Lefamulin can be increased when combined with Oritavancin.
Tazemetostat The metabolism of Tazemetostat can be increased when combined with Oritavancin.
Chlorpromazine The metabolism of Chlorpromazine can be increased when combined with Oritavancin.
Zuclopenthixol The metabolism of Zuclopenthixol can be increased when combined with Oritavancin.

Target Protein

Dihydropteroate synthase folP
Peptidoglycan precursors
Bacterial cell wall peptide bridging segments
Pentaglycyl bridging segment

Referensi & Sumber

Synthesis reference: Adel Rafai Far, Gopal Krishna, Min Ding, Sanjay R, Chemburkar Carl M, Knable James, J. PETZEL, Julie J Pruyne, Douglas M. Reamer.2015. High purity oritavancin and method of producing same.Patent WO2016011245A1
Artikel (PubMed)
  • PMID: 15616289
    Fetterly GJ, Ong CM, Bhavnani SM, Loutit JS, Porter SB, Morello LG, Ambrose PG, Nicolau DP: Pharmacokinetics of oritavancin in plasma and skin blister fluid following administration of a 200-milligram dose for 3 days or a single 800-milligram dose. Antimicrob Agents Chemother. 2005 Jan;49(1):148-52.
  • PMID: 15474317
    Bhavnani SM, Owen JS, Loutit JS, Porter SB, Ambrose PG: Pharmacokinetics, safety, and tolerability of ascending single intravenous doses of oritavancin administered to healthy human subjects. Diagn Microbiol Infect Dis. 2004 Oct;50(2):95-102.
  • PMID: 25709561
    Kmeid J, Kanafani ZA: Oritavancin for the treatment of acute bacterial skin and skin structure infections: an evidence-based review. Core Evid. 2015 Feb 11;10:39-47. doi: 10.2147/CE.S51284. eCollection 2015.
  • PMID: 22664073
    Schuerholz T, Domming S, Hornef M, Dupont A, Kowalski I, Kaconis Y, Heinbockel L, Andra J, Garidel P, Gutsmann T, David S, Sanchez-Gomez S, Martinez de Tejada G, Brandenburg K: Bacterial cell wall compounds as promising targets of antimicrobial agents II. Immunological and clinical aspects. Curr Drug Targets. 2012 Aug;13(9):1131-7. doi: 10.2174/138945012802002438.
  • PMID: 18258256
    Kim SJ, Cegelski L, Stueber D, Singh M, Dietrich E, Tanaka KS, Parr TR Jr, Far AR, Schaefer J: Oritavancin exhibits dual mode of action to inhibit cell-wall biosynthesis in Staphylococcus aureus. J Mol Biol. 2008 Mar 14;377(1):281-93. doi: 10.1016/j.jmb.2008.01.031. Epub 2008 Jan 17.
  • PMID: 22431851
    Zhanel GG, Schweizer F, Karlowsky JA: Oritavancin: mechanism of action. Clin Infect Dis. 2012 Apr;54 Suppl 3:S214-9. doi: 10.1093/cid/cir920.
  • PMID: 25673895
    Cada DJ, Baker DE: Oritavancin diphosphate. Hosp Pharm. 2014 Dec;49(11):1049-60. doi: 10.1310/hjp4911-1049.
  • PMID: 24897083
    Corey GR, Kabler H, Mehra P, Gupta S, Overcash JS, Porwal A, Giordano P, Lucasti C, Perez A, Good S, Jiang H, Moeck G, O'Riordan W: Single-dose oritavancin in the treatment of acute bacterial skin infections. N Engl J Med. 2014 Jun 5;370(23):2180-90. doi: 10.1056/NEJMoa1310422.
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Contoh Produk & Brand

Produk: 6 • International brands: 1
Produk
  • Kimyrsa
    Injection, powder, lyophilized, for solution • 1200 mg/40mL • Intravenous • US • Approved
  • Orbactiv
    Injection, powder, lyophilized, for solution • 400 mg/1 • Intravenous • US • Approved
  • Orbactiv
    Injection, powder, for solution • 400 mg • Intravenous • EU • Approved
  • Orbactiv
    Injection, powder, lyophilized, for solution • 400 mg/1 • Intravenous • US • Approved
  • Orbactiv
    Injection, powder, lyophilized, for solution • 400 mg/1 • Intravenous • US • Approved
  • Tenkasi
    Injection, powder, for solution • 1200 mg • Intravenous • EU • Approved
International Brands
  • Kimyrsa — Melinta Therapeutics, LLC

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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