Peringatan Keamanan

Mice and rats experienced swelling and darkening of exposed tissue at single dosages of >0.85 mg/kg under normal lighting L1128. Systemic toxicity presented as reduced red blood cell and platelet counts and increased white blood cell counts and liver and spleen weights. Skin inflammation, pycnotic spermatocytes and increased extramedullary haematopoiesis in spleen and the lymph nodes was also observed. Under low-light conditions mild phototoxicity was observed only at high doses.

Severe phototoxicity has been seen in rats with repeated doses of up to 1 mg/kg/day under normal lighting L1128. This effect is less severe under low-light conditions. Two weeks of repeated doses of 0.5-0.6 mg/kg/day resulted in inflammation of the injection site and skin in rats. At 0.3 mg/kg/day under low-light in rats, the only effect seen was an increase in white blood cell counts.

In beagle dogs recieving repeated doses of up to 3mg/kg/day under low-light conditions, reddening of the skin and injection site inflammation was seen L1128. Serious injection site damage was observed.

Temoporfin

DB11630

small molecule approved investigational

Deskripsi

Temoporfin is a photosensitizing agent used in the treatment of squamous cell carcinoma of the head and neck FDA Label. It was first authorized for market by the European Medicines Agency in October 2001. It is currently available under the brand name Foscan.

Struktur Molekul 2D

Berat 680.764
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal plasma half life is 65 h [FDA Label]. Elimination of Temoporfin is bi-exponential with the intial phase having a half-life of 30 h and a terminal half-life of 61-88 h [L1128].
Volume Distribusi The volume of distribution is 0.34-0.46 L/kg [L1128]. Temoporfin is known to distribute into the tissues and preferentially collects in tumour tissue.
Klirens (Clearance) Temoporfin is cleared at a rate of 3.9-4.1 mL/h/kg [L1128].

Absorpsi

Tmax is 2-4 h after intravenous administration FDA Label. Plasma concentration initially decreases rapidly then slowly rises to reach peak serum concentration L1128.

Metabolisme

The exact metabolic reactions Temoporfin undergoes are unknown. The drug metabolites have been identified as conjugates but specific information is unavailable.

Rute Eliminasi

Data on elimination in humans is limited FDA Label, L1128. Animal data indicates Temoporfin is eliminated solely by the liver with two conjugated metabolites being excreted through bile. No enterohepatic recirculation has been observed with these metabolites.

Interaksi Obat

42 Data
Porfimer sodium Temoporfin may increase the photosensitizing activities of Porfimer sodium.
Verteporfin Temoporfin may increase the photosensitizing activities of Verteporfin.
Tretinoin The risk or severity of adverse effects can be increased when Tretinoin is combined with Temoporfin.
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Temoporfin.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Temoporfin.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Temoporfin.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Temoporfin.
Padeliporfin Temoporfin may increase the photosensitizing activities of Padeliporfin.
Lidocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Quinisocaine.
Ambroxol The risk or severity of methemoglobinemia can be increased when Temoporfin is combined with Ambroxol.
Etrasimod The risk or severity of immunosuppression can be increased when Temoporfin is combined with Etrasimod.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 10212581
    Hopkinson HJ, Vernon DI, Brown SB: Identification and partial characterization of an unusual distribution of the photosensitizer meta-tetrahydroxyphenyl chlorin (temoporfin) in human plasma. Photochem Photobiol. 1999 Apr;69(4):482-8.
  • PMID: 10529768
    Sharman WM, Allen CM, van Lier JE: Photodynamic therapeutics: basic principles and clinical applications. Drug Discov Today. 1999 Nov;4(11):507-517.
  • PMID: 10487610
    Coutier S, Bezdetnaya L, Marchal S, Melnikova V, Belitchenko I, Merlin JL, Guillemin F: Foscan (mTHPC) photosensitized macrophage activation: enhancement of phagocytosis, nitric oxide release and tumour necrosis factor-alpha-mediated cytolytic activity. Br J Cancer. 1999 Sep;81(1):37-42. doi: 10.1038/sj.bjc.6690648.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Foscan
    Injection, solution • 1 mg/ml • Intravenous • EU • Approved
  • Foscan
    Injection, solution • 1 mg/ml • Intravenous • EU • Approved
  • Foscan
    Injection, solution • 1 mg/ml • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

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