Laquinimod

DB06685

small molecule investigational

Deskripsi

Laquinimod is an immunomodulator developed by Active Biotech and produced by Teva Pharmaceutical Industries. It is currently under development in phase III trials for treatment of multiple sclerosis as an oral therapy, like fingolimod. It has been shown to reduce disease activity on magnetic resonance imaging and to be well tolerated orally.

Struktur Molekul 2D

Berat 356.81
Wujud solid

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

Profil Farmakokinetik

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

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Hepatic. Cytochrome P450 3A4 is the major enzyme responsible for the metabolism of laquinimod.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

106 Data
Pitolisant The serum concentration of Laquinimod can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Laquinimod can be increased when combined with Metreleptin.
Cenobamate The serum concentration of Laquinimod can be decreased when it is combined with Cenobamate.
Ritonavir The serum concentration of Laquinimod can be increased when it is combined with Ritonavir.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Laquinimod.
Tucatinib The metabolism of Tucatinib can be decreased when combined with Laquinimod.
Abametapir The serum concentration of Laquinimod can be increased when it is combined with Abametapir.
Satralizumab The serum concentration of Laquinimod can be decreased when it is combined with Satralizumab.
Sotorasib The serum concentration of Laquinimod can be decreased when it is combined with Sotorasib.
Cyclosporine The metabolism of Laquinimod can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Laquinimod can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Laquinimod can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Laquinimod can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Laquinimod can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Laquinimod can be decreased when combined with Isradipine.
Diltiazem The metabolism of Laquinimod can be decreased when combined with Diltiazem.
Clozapine The metabolism of Laquinimod can be decreased when combined with Clozapine.
Ciprofloxacin The metabolism of Laquinimod can be decreased when combined with Ciprofloxacin.
Nicardipine The metabolism of Laquinimod can be decreased when combined with Nicardipine.
Verapamil The metabolism of Laquinimod can be decreased when combined with Verapamil.
Aprepitant The metabolism of Laquinimod can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Laquinimod can be decreased when combined with Isoniazid.
Primaquine The metabolism of Laquinimod can be decreased when combined with Primaquine.
Miconazole The metabolism of Laquinimod can be decreased when combined with Miconazole.
Fusidic acid The metabolism of Laquinimod can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Laquinimod can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Laquinimod can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Laquinimod can be decreased when combined with Milnacipran.
Simeprevir The metabolism of Laquinimod can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Laquinimod can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Laquinimod can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Laquinimod can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Laquinimod can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Laquinimod can be decreased when combined with Linagliptin.
Indalpine The metabolism of Laquinimod can be decreased when combined with Indalpine.
Netupitant The metabolism of Laquinimod can be decreased when combined with Netupitant.
Barnidipine The metabolism of Laquinimod can be decreased when combined with Barnidipine.
Benidipine The metabolism of Laquinimod can be decreased when combined with Benidipine.
Venetoclax The metabolism of Laquinimod can be decreased when combined with Venetoclax.
Isavuconazole The metabolism of Laquinimod can be decreased when combined with Isavuconazole.
Fosnetupitant The metabolism of Laquinimod can be decreased when combined with Fosnetupitant.
Berotralstat The metabolism of Laquinimod can be decreased when combined with Berotralstat.
Midostaurin The metabolism of Laquinimod can be decreased when combined with Midostaurin.
Voriconazole The metabolism of Laquinimod can be decreased when combined with Voriconazole.
Danazol The metabolism of Laquinimod can be decreased when combined with Danazol.
Nelfinavir The metabolism of Laquinimod can be decreased when combined with Nelfinavir.
Indinavir The metabolism of Laquinimod can be decreased when combined with Indinavir.
Terfenadine The metabolism of Laquinimod can be decreased when combined with Terfenadine.
Efavirenz The metabolism of Laquinimod can be decreased when combined with Efavirenz.
Ergotamine The metabolism of Laquinimod can be decreased when combined with Ergotamine.
Amprenavir The metabolism of Laquinimod can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Laquinimod can be decreased when combined with Delavirdine.
Methimazole The metabolism of Laquinimod can be decreased when combined with Methimazole.
Conivaptan The metabolism of Laquinimod can be decreased when combined with Conivaptan.
Tipranavir The metabolism of Laquinimod can be decreased when combined with Tipranavir.
Telithromycin The metabolism of Laquinimod can be decreased when combined with Telithromycin.
Ketoconazole The metabolism of Laquinimod can be decreased when combined with Ketoconazole.
Atazanavir The metabolism of Laquinimod can be decreased when combined with Atazanavir.
Amiodarone The metabolism of Laquinimod can be decreased when combined with Amiodarone.
Nefazodone The metabolism of Laquinimod can be decreased when combined with Nefazodone.
Itraconazole The metabolism of Laquinimod can be decreased when combined with Itraconazole.
Clarithromycin The metabolism of Laquinimod can be decreased when combined with Clarithromycin.
Saquinavir The metabolism of Laquinimod can be decreased when combined with Saquinavir.
Posaconazole The metabolism of Laquinimod can be decreased when combined with Posaconazole.
Darunavir The metabolism of Laquinimod can be decreased when combined with Darunavir.
Lopinavir The metabolism of Laquinimod can be decreased when combined with Lopinavir.
Ditiocarb The metabolism of Laquinimod can be decreased when combined with Ditiocarb.
Nilotinib The metabolism of Laquinimod can be decreased when combined with Nilotinib.
Telaprevir The metabolism of Laquinimod can be decreased when combined with Telaprevir.
Lonafarnib The metabolism of Laquinimod can be decreased when combined with Lonafarnib.
Boceprevir The metabolism of Laquinimod can be decreased when combined with Boceprevir.
Elvitegravir The metabolism of Laquinimod can be decreased when combined with Elvitegravir.
Stiripentol The metabolism of Laquinimod can be decreased when combined with Stiripentol.
Ribociclib The metabolism of Laquinimod can be decreased when combined with Ribociclib.
Danoprevir The metabolism of Laquinimod can be decreased when combined with Danoprevir.
Troleandomycin The metabolism of Laquinimod can be decreased when combined with Troleandomycin.
Phenytoin The metabolism of Laquinimod can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Laquinimod can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Laquinimod can be increased when combined with Carbamazepine.
Mitotane The metabolism of Laquinimod can be increased when combined with Mitotane.
Primidone The metabolism of Laquinimod can be increased when combined with Primidone.
Rifampin The metabolism of Laquinimod can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Laquinimod can be increased when combined with Phenobarbital.
Dexamethasone The metabolism of Laquinimod can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Laquinimod can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Laquinimod can be increased when combined with St. John's Wort.
Enzalutamide The serum concentration of Laquinimod can be decreased when it is combined with Enzalutamide.
Lumacaftor The metabolism of Laquinimod can be increased when combined with Lumacaftor.
Apalutamide The serum concentration of Laquinimod can be decreased when it is combined with Apalutamide.
Rifapentine The metabolism of Laquinimod can be increased when combined with Rifapentine.
Curcumin The metabolism of Laquinimod can be decreased when combined with Curcumin.
Somatrogon The metabolism of Laquinimod can be increased when combined with Somatrogon.
Levoketoconazole The metabolism of Laquinimod can be decreased when combined with Levoketoconazole.
Mavacamten The serum concentration of Laquinimod can be decreased when it is combined with Mavacamten.
Viloxazine The metabolism of Laquinimod can be decreased when combined with Viloxazine.
Ivosidenib The metabolism of Laquinimod can be increased when combined with Ivosidenib.
Dabrafenib The serum concentration of Laquinimod can be decreased when it is combined with Dabrafenib.
Telotristat ethyl The serum concentration of Laquinimod can be decreased when it is combined with Telotristat ethyl.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Laquinimod.
Omaveloxolone The serum concentration of Laquinimod can be decreased when it is combined with Omaveloxolone.

Target Protein

Transcription factor RelB RELB
Nuclear factor NF-kappa-B p105 subunit NFKB1
Nuclear factor NF-kappa-B p100 subunit NFKB2
Transcription factor p65 RELA
Proto-oncogene c-Rel REL
C-X-C motif chemokine 2 CXCL2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15764719
    Tuvesson H, Hallin I, Persson R, Sparre B, Gunnarsson PO, Seidegard J: Cytochrome P450 3A4 is the major enzyme responsible for the metabolism of laquinimod, a novel immunomodulator. Drug Metab Dispos. 2005 Jun;33(6):866-72. Epub 2005 Mar 11.
  • PMID: 18572078
    Comi G, Pulizzi A, Rovaris M, Abramsky O, Arbizu T, Boiko A, Gold R, Havrdova E, Komoly S, Selmaj K, Sharrack B, Filippi M: Effect of laquinimod on MRI-monitored disease activity in patients with relapsing-remitting multiple sclerosis: a multicentre, randomised, double-blind, placebo-controlled phase IIb study. Lancet. 2008 Jun 21;371(9630):2085-92. doi: 10.1016/S0140-6736(08)60918-6.
  • PMID: 15465591
    Yang JS, Xu LY, Xiao BG, Hedlund G, Link H: Laquinimod (ABR-215062) suppresses the development of experimental autoimmune encephalomyelitis, modulates the Th1/Th2 balance and induces the Th3 cytokine TGF-beta in Lewis rats. J Neuroimmunol. 2004 Nov;156(1-2):3-9.

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Sekuens Gen/Protein (FASTA)

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