Minimum lethal dose in rat: 500 mg/kg.
Maximum asymptomatic dose in non human primate: 40 mg/kg.
Lymphatic, immune system, bone marrow and erythroid cell toxicity was seen in animal studies involving rate and monkeys. Doses used in these studies ranged from 1mg/kg/day to 10mg/kg/day, over a duration of 6 weeks to 6 months. Lymphopenia, neutropenia, and anemia is seen in human subjects and may call for an interruption or discontinuation of therapy if severe.
Reduced female fertility in rats was seen at exposures 17 times the maximum recommended human dose. Fertility may be impaired in human females and harm may be caused to unborn child.
Carcinogenic potential is seen, however evidence for dose dependency is lacking.
Because the janus kinase pathway plays a role in stimulating the production of red blood cells and is involved in immune cell function, inhibition of this pathway leads to increased risk of anemia, neutropenia, lymphopenia, cancer and infection.
Lymphopenia, neutropenia, and anemia in human subjects may call for an interruption or discontinuation of therapy if severe.
Role of JAK inhibition in the development of gastrointestinal perforation is not known.
Tofacitinib is an inhibitor of Janus kinases, a group of intracellular enzymes involved in signalling pathways that affect hematopoiesis and immune cell function. It is approved by the FDA for treatment of moderate to severe rheumatoid arthritis that responds inadequately to methotrexate or in those who are intolerant to methotrexate.
Besides rheumatoid arthritis, tofacitinib has also been studied in clinical trials for the prevention of organ transplant rejection, and is currently under investigation for the treatment of psoriasis. Known adverse effects include nausea and headache as well as more serious immunologic and hematological adverse effects. Tofacitinib is marketed under the brand name Xeljanz by Pfizer.
Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).
drugbank-id dan name pada skema XML DrugBank.targets/target yang memuat polipeptida sasaran.gene-name dan varian snp-effects.Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.
| Denosumab | The risk or severity of adverse effects can be increased when Denosumab is combined with Tofacitinib. |
| Methotrexate | The risk or severity of adverse effects can be increased when Methotrexate is combined with Tofacitinib. |
| Sulfasalazine | The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Tofacitinib. |
| Hydroxychloroquine | The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Tofacitinib. |
| Natalizumab | The risk or severity of immunosuppression can be increased when Tofacitinib is combined with Natalizumab. |
| Pimecrolimus | The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tofacitinib. |
| Roflumilast | Roflumilast may increase the immunosuppressive activities of Tofacitinib. |
| Sipuleucel-T | The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Tofacitinib. |
| Anakinra | The risk or severity of adverse effects can be increased when Anakinra is combined with Tofacitinib. |
| Rituximab | Rituximab may increase the immunosuppressive activities of Tofacitinib. |
| Ceritinib | Tofacitinib may increase the bradycardic activities of Ceritinib. |
| Ivabradine | Tofacitinib may increase the bradycardic activities of Ivabradine. |
| Fluconazole | The metabolism of Tofacitinib can be decreased when combined with Fluconazole. |
| Clozapine | The metabolism of Tofacitinib can be decreased when combined with Clozapine. |
| Aldesleukin | The metabolism of Tofacitinib can be decreased when combined with Aldesleukin. |
| Octreotide | The metabolism of Tofacitinib can be decreased when combined with Octreotide. |
| Fluvoxamine | The metabolism of Tofacitinib can be decreased when combined with Fluvoxamine. |
| Erythromycin | The metabolism of Tofacitinib can be decreased when combined with Erythromycin. |
| Citalopram | The metabolism of Tofacitinib can be decreased when combined with Citalopram. |
| Nelfinavir | The metabolism of Tofacitinib can be decreased when combined with Nelfinavir. |
| Indinavir | The metabolism of Tofacitinib can be decreased when combined with Indinavir. |
| Ziprasidone | The metabolism of Tofacitinib can be decreased when combined with Ziprasidone. |
| Cabergoline | The metabolism of Tofacitinib can be decreased when combined with Cabergoline. |
| Diethylstilbestrol | The metabolism of Tofacitinib can be decreased when combined with Diethylstilbestrol. |
| Isradipine | The metabolism of Tofacitinib can be decreased when combined with Isradipine. |
| Valproic acid | The metabolism of Tofacitinib can be decreased when combined with Valproic acid. |
| Acetaminophen | The metabolism of Tofacitinib can be decreased when combined with Acetaminophen. |
| Dihydroergotamine | The metabolism of Tofacitinib can be decreased when combined with Dihydroergotamine. |
| Methadone | The metabolism of Tofacitinib can be decreased when combined with Methadone. |
| Terfenadine | The metabolism of Tofacitinib can be decreased when combined with Terfenadine. |
| Diltiazem | The metabolism of Tofacitinib can be decreased when combined with Diltiazem. |
| Methylergometrine | The metabolism of Tofacitinib can be decreased when combined with Methylergometrine. |
| Mefloquine | The metabolism of Tofacitinib can be decreased when combined with Mefloquine. |
| Mirtazapine | The metabolism of Tofacitinib can be decreased when combined with Mirtazapine. |
| Sorafenib | The metabolism of Tofacitinib can be decreased when combined with Sorafenib. |
| Nitric Oxide | The metabolism of Tofacitinib can be decreased when combined with Nitric Oxide. |
| Cerivastatin | The metabolism of Tofacitinib can be decreased when combined with Cerivastatin. |
| Teniposide | The metabolism of Tofacitinib can be decreased when combined with Teniposide. |
| Chloramphenicol | The metabolism of Tofacitinib can be decreased when combined with Chloramphenicol. |
| Lansoprazole | The metabolism of Tofacitinib can be decreased when combined with Lansoprazole. |
| Quinine | The metabolism of Tofacitinib can be decreased when combined with Quinine. |
| Raloxifene | The metabolism of Tofacitinib can be decreased when combined with Raloxifene. |
| Cimetidine | The metabolism of Tofacitinib can be decreased when combined with Cimetidine. |
| Haloperidol | The metabolism of Tofacitinib can be decreased when combined with Haloperidol. |
| Ritonavir | The metabolism of Tofacitinib can be decreased when combined with Ritonavir. |
| Erlotinib | The metabolism of Tofacitinib can be decreased when combined with Erlotinib. |
| Ciprofloxacin | The metabolism of Tofacitinib can be decreased when combined with Ciprofloxacin. |
| Zafirlukast | The metabolism of Tofacitinib can be decreased when combined with Zafirlukast. |
| Vinblastine | The metabolism of Tofacitinib can be decreased when combined with Vinblastine. |
| Fluticasone propionate | The metabolism of Tofacitinib can be decreased when combined with Fluticasone propionate. |
| Thiopental | The metabolism of Tofacitinib can be decreased when combined with Thiopental. |
| Imatinib | The metabolism of Tofacitinib can be decreased when combined with Imatinib. |
| Nicardipine | The metabolism of Tofacitinib can be decreased when combined with Nicardipine. |
| Efavirenz | The metabolism of Tofacitinib can be decreased when combined with Efavirenz. |
| Astemizole | The metabolism of Tofacitinib can be decreased when combined with Astemizole. |
| Dextropropoxyphene | The metabolism of Tofacitinib can be decreased when combined with Dextropropoxyphene. |
| Verapamil | The metabolism of Tofacitinib can be decreased when combined with Verapamil. |
| Epinephrine | The metabolism of Tofacitinib can be decreased when combined with Epinephrine. |
| Aprepitant | The metabolism of Tofacitinib can be decreased when combined with Aprepitant. |
| Tamoxifen | The metabolism of Tofacitinib can be decreased when combined with Tamoxifen. |
| Midazolam | The metabolism of Tofacitinib can be decreased when combined with Midazolam. |
| Daunorubicin | The metabolism of Tofacitinib can be decreased when combined with Daunorubicin. |
| Ergotamine | The metabolism of Tofacitinib can be decreased when combined with Ergotamine. |
| Amprenavir | The metabolism of Tofacitinib can be decreased when combined with Amprenavir. |
| Delavirdine | The metabolism of Tofacitinib can be decreased when combined with Delavirdine. |
| Paroxetine | The metabolism of Tofacitinib can be decreased when combined with Paroxetine. |
| Tranylcypromine | The metabolism of Tofacitinib can be decreased when combined with Tranylcypromine. |
| Tetracycline | The metabolism of Tofacitinib can be decreased when combined with Tetracycline. |
| Methimazole | The metabolism of Tofacitinib can be decreased when combined with Methimazole. |
| Roxithromycin | The metabolism of Tofacitinib can be decreased when combined with Roxithromycin. |
| Phenelzine | The metabolism of Tofacitinib can be decreased when combined with Phenelzine. |
| Propofol | The metabolism of Tofacitinib can be decreased when combined with Propofol. |
| Acetazolamide | The metabolism of Tofacitinib can be decreased when combined with Acetazolamide. |
| Diazepam | The metabolism of Tofacitinib can be decreased when combined with Diazepam. |
| Mifepristone | The metabolism of Tofacitinib can be decreased when combined with Mifepristone. |
| Loperamide | Loperamide may increase the bradycardic activities of Tofacitinib. |
| Clofazimine | The metabolism of Tofacitinib can be decreased when combined with Clofazimine. |
| Tacrolimus | The metabolism of Tofacitinib can be decreased when combined with Tacrolimus. |
| Conivaptan | The metabolism of Tofacitinib can be decreased when combined with Conivaptan. |
| Ethanol | The metabolism of Tofacitinib can be decreased when combined with Ethanol. |
| Quinidine | The metabolism of Tofacitinib can be decreased when combined with Quinidine. |
| Metronidazole | The metabolism of Tofacitinib can be decreased when combined with Metronidazole. |
| Buprenorphine | The metabolism of Tofacitinib can be decreased when combined with Buprenorphine. |
| Tipranavir | The metabolism of Tofacitinib can be decreased when combined with Tipranavir. |
| Isoniazid | The metabolism of Tofacitinib can be decreased when combined with Isoniazid. |
| Dirithromycin | The metabolism of Tofacitinib can be decreased when combined with Dirithromycin. |
| Telithromycin | The metabolism of Tofacitinib can be decreased when combined with Telithromycin. |
| Doxorubicin | The metabolism of Tofacitinib can be decreased when combined with Doxorubicin. |
| Metyrapone | The metabolism of Tofacitinib can be decreased when combined with Metyrapone. |
| Glyburide | The metabolism of Tofacitinib can be decreased when combined with Glyburide. |
| Ketoconazole | The metabolism of Tofacitinib can be decreased when combined with Ketoconazole. |
| Irbesartan | The metabolism of Tofacitinib can be decreased when combined with Irbesartan. |
| Topotecan | The metabolism of Tofacitinib can be decreased when combined with Topotecan. |
| Norfloxacin | The metabolism of Tofacitinib can be decreased when combined with Norfloxacin. |
| Oxybutynin | The metabolism of Tofacitinib can be decreased when combined with Oxybutynin. |
| Mequitazine | The metabolism of Tofacitinib can be decreased when combined with Mequitazine. |
| Atazanavir | The metabolism of Tofacitinib can be decreased when combined with Atazanavir. |
| Primaquine | The metabolism of Tofacitinib can be decreased when combined with Primaquine. |
| Dimethyl sulfoxide | The metabolism of Tofacitinib can be decreased when combined with Dimethyl sulfoxide. |
| Fluvastatin | The metabolism of Tofacitinib can be decreased when combined with Fluvastatin. |