Peringatan Keamanan

The oral LD50 in rats is 113 mg/kg and 2 g/kg in mouse.L41330

Two-year carcinogenicity studies were conducted in male and female rats and mice. No compound-related tumorigenic effects were observed at the highest dose levels of 3,000 mg/kg/day to male and female mice (38-fold greater than the highest recommended daily human dose of 400 mg based upon body surface area BSA), 3,000 mg/kg/day to female rats (75-fold the maximum human dose based upon BSA), and 300 mg/kg/day to male rats (7.5-fold the maximum human dose based upon BSA). L41235

Thalidomide was neither mutagenic nor genotoxic in the following assays: the Ames bacterial (S. typhimurium and E. coli) reverse mutation assay, a Chinese hamster ovary cell (AS52/XPRT) forward mutation assay, and an in vivo mouse micronucleus test. L41235

Fertility studies were conducted in male and female rabbits; no compound-related effects in mating and fertility indices were observed at any oral thalidomide dose level including the highest of 100 mg/kg/day to female rabbits and 500 mg/kg/day to male rabbits (approximately 5- and 25- fold the maximum human dose, respectively, based upon BSA). Testicular pathological and histopathological effects (classified as slight) were seen in male rabbits at dose levels ?30 mg/kg/day (approximately 1.5-fold the maximum human dose based upon BSA). L41235

There is no specific antidote for a thalidomide overdose. In the event of an overdose, the patient’s vital signs should be monitored and appropriate supportive care given to maintain blood pressure and respiratory status. L41235

Thalidomide

DB01041

small molecule approved investigational withdrawn

Deskripsi

A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, thalidomide was withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of inflammatory disorders and cancers. Thalidomide displays immunosuppressive and anti-angiogenic activity through modulating the release of inflammatory mediators like tumor necrosis factor-alpha (TNF-a) and other cytokine action. Due to severe teratogenicity, pregnancy must be excluded before the start of treatment and patients must enrol in the THALIDOMID Risk Evaluation and Mitigation Strategy (REMS) program to ensure contraception adherence.L41235

Struktur Molekul 2D

Berat 258.2295
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of thalidomide in healthy male subjects after a single dose of 200 mg is 6.17 ± 2.56 h. [A246130]
Volume Distribusi The volume of distribution of thalidomide is difficult to determine due to spontaneous hydrolysis and chiral inversion, but it is estimated to be 70-120 L. [A246135,A246140]
Klirens (Clearance) The oral clearance of thalidomide is 10.50 ± 2.10 L/h. [A246130]

Absorpsi

The absolute bioavailability has not yet been characterized in human subjects due to its poor aqueous solubility. The mean time to peak plasma concentrations (Tmax) ranged from 2.9 to 5.7 hours following a single dose from 50 to 400 mg. Patients with Hansen’s disease may have an increased bioavailability of thalidomide, although the clinical significance of this is unknown. L41235 Due to its low aqueous solubility and thus low dissolution is the gastrointestinal tract, thalidomide's absorption is slow, with a tlag of 20-40 min. Therefore, thalidomide exhibits absorption rate-limited pharmacokinetics or "flip-flop" phenomenon. Following a single dose of 200 mg in healthy male subjects, cmax and AUC? were calculated to be 2.00 ± 0.55 mg/L and 19.80 ± 3.61 mg*h/mL respectively. A246135

Metabolisme

Thalidomide appears to undergo primarily non-enzymatic hydrolysis in plasma to multiple metabolites, as the four amide bonds in thalidomide allow for rapid hydrolysis under physiological pH. A246130 Evidences for enzymatic metabolism of thalidomide is mixed, as in vitro studies using rat liver microsome have detected 5-hydroxythalidomide (5-OH), a monohydroxylated metabolite of thalidomide catalyzed by the CYP2C19 enzyme, and the addition of omeprazole, a CYP2C19 inhibitor, inhibits the metabolism of thalidomide. A246130 5-hydroxythalidomide (5-OH) has also been detected in the plasma of 32% of androgen-independent prostate cancer patients undergoing oral thalidomide treatment.A246130 However, significant interspecies difference in thalidomide metabolism has been noted, potentially signifying that animals like rats and rabbits rely on enzymatic metabolism of thalidomide more than human.A246130

Rute Eliminasi

Thalidomide is primarily excreted in urine as hydrolytic metabolites since less than 1% of the parent form is detected in the urine. Fecal excretion of thalidomide is minimal. L41235

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Ingesting alcohol may increase the drowsiness caused by thalidomide.
  • 2. Take after a meal. Wait at least 1 hour after eating before taking thalidomide.

Interaksi Obat

1785 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Thalidomide.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Thalidomide.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Thalidomide.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Thalidomide.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Thalidomide.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Thalidomide.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Thalidomide.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Thalidomide.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Thalidomide.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Thalidomide.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Thalidomide.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Thalidomide.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Thalidomide.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Thalidomide.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Thalidomide.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Thalidomide.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Thalidomide.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Thalidomide.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Thalidomide.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Thalidomide.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Thalidomide.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Thalidomide.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Thalidomide.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Thalidomide.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Thalidomide.
Bortezomib The risk or severity of peripheral neuropathy can be increased when Thalidomide is combined with Bortezomib.
Cladribine Thalidomide may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Thalidomide.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Thalidomide.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Thalidomide.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Thalidomide.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Thalidomide.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Thalidomide.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Thalidomide.
Vindesine The metabolism of Vindesine can be increased when combined with Thalidomide.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Thalidomide.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Thalidomide.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Thalidomide.
Vinorelbine The metabolism of Vinorelbine can be increased when combined with Thalidomide.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Thalidomide.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Thalidomide.
Sorafenib The metabolism of Sorafenib can be increased when combined with Thalidomide.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Thalidomide.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Thalidomide.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Thalidomide.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Thalidomide.
Teniposide The metabolism of Teniposide can be increased when combined with Thalidomide.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Thalidomide.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Thalidomide.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Thalidomide.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Thalidomide.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Thalidomide.
Cisplatin The risk or severity of peripheral neuropathy can be increased when Thalidomide is combined with Cisplatin.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Thalidomide.
Vincristine The risk or severity of peripheral neuropathy can be increased when Thalidomide is combined with Vincristine.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Thalidomide.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Thalidomide.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Thalidomide.
Methotrexate The metabolism of Methotrexate can be increased when combined with Thalidomide.
Vinblastine The metabolism of Vinblastine can be increased when combined with Thalidomide.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Thalidomide.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Thalidomide.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Thalidomide.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Thalidomide.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Thalidomide.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Thalidomide.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Thalidomide.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Thalidomide.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Thalidomide.
Tretinoin The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Thalidomide.
Irinotecan The metabolism of Irinotecan can be increased when combined with Thalidomide.
Methimazole The metabolism of Thalidomide can be decreased when combined with Methimazole.
Etoposide The metabolism of Etoposide can be increased when combined with Thalidomide.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Thalidomide.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Thalidomide.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Thalidomide.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Thalidomide.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Thalidomide.
Sirolimus The metabolism of Sirolimus can be increased when combined with Thalidomide.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Thalidomide.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Thalidomide.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Thalidomide.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Thalidomide.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Thalidomide.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Thalidomide.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Thalidomide.
Doxorubicin The serum concentration of Doxorubicin can be decreased when it is combined with Thalidomide.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Thalidomide.
Busulfan The metabolism of Busulfan can be increased when combined with Thalidomide.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Thalidomide.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Thalidomide.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Thalidomide is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Thalidomide is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Thalidomide is combined with Flucytosine.
Trilostane The risk or severity of adverse effects can be increased when Thalidomide is combined with Trilostane.
Arsenic trioxide The risk or severity of adverse effects can be increased when Thalidomide is combined with Arsenic trioxide.
Idarubicin The risk or severity of adverse effects can be increased when Thalidomide is combined with Idarubicin.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Thalidomide.
Estramustine The risk or severity of adverse effects can be increased when Thalidomide is combined with Estramustine.

Target Protein

Tumor necrosis factor TNF
Protein cereblon CRBN
DNA
alpha1-acid glycoprotein ORM1

Referensi & Sumber

Synthesis reference: Jamshed Shah, "Synthesis and anti-tumor activity of nitrogen substituted thalidomide analogs." U.S. Patent US20030139451, issued July 24, 2003.
Artikel (PubMed)
  • PMID: 11599654
    Eriksson T, Bjorkman S, Hoglund P: Clinical pharmacology of thalidomide. Eur J Clin Pharmacol. 2001 Aug;57(5):365-76. doi: 10.1007/s002280100320.
  • PMID: 24292625
    Kronke J, Udeshi ND, Narla A, Grauman P, Hurst SN, McConkey M, Svinkina T, Heckl D, Comer E, Li X, Ciarlo C, Hartman E, Munshi N, Schenone M, Schreiber SL, Carr SA, Ebert BL: Lenalidomide causes selective degradation of IKZF1 and IKZF3 in multiple myeloma cells. Science. 2014 Jan 17;343(6168):301-5. doi: 10.1126/science.1244851. Epub 2013 Nov 29.
  • PMID: 16918319
    Lepper ER, Smith NF, Cox MC, Scripture CD, Figg WD: Thalidomide metabolism and hydrolysis: mechanisms and implications. Curr Drug Metab. 2006 Aug;7(6):677-85. doi: 10.2174/138920006778017777.
  • PMID: 15080764
    Teo SK, Colburn WA, Tracewell WG, Kook KA, Stirling DI, Jaworsky MS, Scheffler MA, Thomas SD, Laskin OL: Clinical pharmacokinetics of thalidomide. Clin Pharmacokinet. 2004;43(5):311-27. doi: 10.2165/00003088-200443050-00004.
  • PMID: 16344099
    Anderson KC: Lenalidomide and thalidomide: mechanisms of action--similarities and differences. Semin Hematol. 2005 Oct;42(4 Suppl 4):S3-8.
  • PMID: 12197242
    Baidas S, Tfayli A, Bhargava P: Thalidomide: an old drug with new clinical applications. Cancer Invest. 2002;20(5-6):835-48. doi: 10.1081/cnv-120002498.
  • PMID: 30459439
    Tokunaga E, Yamamoto T, Ito E, Shibata N: Understanding the Thalidomide Chirality in Biological Processes by the Self-disproportionation of Enantiomers. Sci Rep. 2018 Nov 20;8(1):17131. doi: 10.1038/s41598-018-35457-6.
  • PMID: 22650377
    Majumder S, Sreedhara SR, Banerjee S, Chatterjee S: TNF alpha signaling beholds thalidomide saga: a review of mechanistic role of TNF-alpha signaling under thalidomide. Curr Top Med Chem. 2012;12(13):1456-67. doi: 10.2174/156802612801784443.
Menampilkan 8 dari 9 artikel.

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