Peringatan Keamanan

There is no information available regarding the acute toxicity (LD50) or overdose of zilucoplan.L48516

Zilucoplan

DB15636

small molecule approved

Deskripsi

Zilucoplan is a 15 amino-acid, synthetic macrocyclic peptide. It is a complement inhibitor that works to prevent the activation of C5, which is a complement protein involved in the innate immune system to initiate inflammatory responses.A261841 On October 17, 2023, zilucoplan gained its first FDA approval for the treatment of generalized myasthenia gravis.L48701 It was also later approved by the EMA on December 4, 2023, as an add-on treatment for the same condition.L49131

Struktur Molekul 2D

Berat 3562.229
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean plasma terminal half-life of zilucoplan was approximately 172 hours (7 to 8 days).[L48516]
Volume Distribusi The mean volume of distribution at steady state was 3.51 L in the population pharmacokinetics analysis for adult patients with gMG.[L48516]
Klirens (Clearance) No information is available.

Absorpsi

Following single and multiple daily subcutaneous administration of 0.3 mg/kg zilucoplan, time to reach peak plasma concentrations (Tmax) ranged from three to six hours. Following daily subcutaneous dosing of 0.3 mg/kg zilucoplan for 14 days in healthy subjects, both the peak plasma concentration and exposure (AUCtau) increased by approximately 3-fold.L48516 After daily repeated subcutaneous administration of 0.3 mg/kg zilucoplan, plasma concentrations of zilucoplan were consistent, with steady state trough concentrations being reached by four weeks of treatment with zilucoplan through 12 weeks.L48516

Metabolisme

Zilucoplan is expected to be degraded into small peptides and amino acids via catabolic pathways. RA103488 and RA102758 are two major metabolites detected in plasma. RA103488 is formed by CYP4F2-mediated metabolism and has comparable pharmacological activity to its parent compound; however, since RA103488 is present at much lower concentrations compared to zilucoplan, its contribution to the pharmacological action of zilucoplan is expected to be low. RA102758, formed by protease-mediated degradation, is pharmacologically inactive. The AUCs of both metabolites were approximately 10% of the parent AUC.L48516

Rute Eliminasi

Less than 1% of zilucoplan and its metabolites are excreted in urine and feces.L48516

Interaksi Obat

353 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Zilucoplan.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Zilucoplan.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Zilucoplan.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Zilucoplan.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Zilucoplan.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Zilucoplan.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Zilucoplan.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Zilucoplan.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Zilucoplan.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Zilucoplan.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Zilucoplan.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Zilucoplan.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Zilucoplan.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Zilucoplan.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Zilucoplan.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Zilucoplan.
Trastuzumab The risk or severity of neutropenia can be increased when Trastuzumab is combined with Zilucoplan.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Zilucoplan.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Zilucoplan.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Zilucoplan.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Zilucoplan.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Zilucoplan.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Zilucoplan.
Cyclosporine Zilucoplan may increase the immunosuppressive activities of Cyclosporine.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Zilucoplan.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Zilucoplan.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Zilucoplan.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Zilucoplan.
Natalizumab The risk or severity of immunosuppression can be increased when Zilucoplan is combined with Natalizumab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Zilucoplan.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Zilucoplan.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Zilucoplan.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Zilucoplan.
Cladribine Zilucoplan may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Zilucoplan.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Zilucoplan.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Zilucoplan.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Zilucoplan.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Zilucoplan.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Zilucoplan.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Zilucoplan.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Zilucoplan.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Zilucoplan.
Fluorometholone The risk or severity of adverse effects can be increased when Fluorometholone is combined with Zilucoplan.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Zilucoplan.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Zilucoplan.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Zilucoplan.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Zilucoplan.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Zilucoplan.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Zilucoplan.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Zilucoplan.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Zilucoplan.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Zilucoplan.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Zilucoplan.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Zilucoplan.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Zilucoplan.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Zilucoplan.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Zilucoplan.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Zilucoplan.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Zilucoplan.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Zilucoplan.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Zilucoplan.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Zilucoplan.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Zilucoplan.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Zilucoplan.
Desoximetasone The risk or severity of adverse effects can be increased when Desoximetasone is combined with Zilucoplan.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Zilucoplan.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Zilucoplan.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Zilucoplan.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Zilucoplan.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Zilucoplan.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Zilucoplan.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Zilucoplan.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Zilucoplan.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Zilucoplan.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Zilucoplan.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Zilucoplan.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Zilucoplan.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Zilucoplan.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Zilucoplan.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Zilucoplan.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Zilucoplan.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Zilucoplan.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Zilucoplan.
Mometasone The risk or severity of adverse effects can be increased when Mometasone is combined with Zilucoplan.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Zilucoplan.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Zilucoplan.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Zilucoplan.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Zilucoplan.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Zilucoplan.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Zilucoplan.
Tacrolimus Tacrolimus may increase the immunosuppressive activities of Zilucoplan.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Zilucoplan.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Zilucoplan.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Zilucoplan.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Zilucoplan.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Zilucoplan.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Zilucoplan.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Zilucoplan.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Zilucoplan.

Target Protein

Complement C5 C5

Referensi & Sumber

Artikel (PubMed)
  • PMID: 37622108
    Tang GQ, Tang Y, Dhamnaskar K, Hoarty MD, Vyasamneni R, Vadysirisack DD, Ma Z, Zhu N, Wang JG, Bu C, Cong B, Palmer E, Duda PW, Sayegh C, Ricardo A: Zilucoplan, a macrocyclic peptide inhibitor of human complement component 5, uses a dual mode of action to prevent terminal complement pathway activation. Front Immunol. 2023 Aug 9;14:1213920. doi: 10.3389/fimmu.2023.1213920. eCollection 2023.
  • PMID: 35639288
    Menon D, Bril V: Pharmacotherapy of Generalized Myasthenia Gravis with Special Emphasis on Newer Biologicals. Drugs. 2022 Jun;82(8):865-887. doi: 10.1007/s40265-022-01726-y. Epub 2022 May 31.
  • PMID: 33792453
    Howard JF Jr, Vissing J, Gilhus NE, Leite MI, Utsugisawa K, Duda PW, Farzaneh-Far R, Murai H, Wiendl H: Zilucoplan: An Investigational Complement C5 Inhibitor for the Treatment of Acetylcholine Receptor Autoantibody-Positive Generalized Myasthenia Gravis. Expert Opin Investig Drugs. 2021 May;30(5):483-493. doi: 10.1080/13543784.2021.1897567. Epub 2021 Apr 1.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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