Peringatan Keamanan

Data regarding overdoses in humans are not readily available.L34095 In the case of an overdose, patients should be treated with symptomatic and supportive measures.

Pegcetacoplan

DB16694

biotech approved

Deskripsi

Pegcetacoplan is a complement inhibitor indicated in the treatment of paroxysmal nocturnal hemoglobinuria (PNH).A235000,L34095 Prior to its FDA approval, patients with PNH were typically treated with the C5 inhibiting monoclonal antibody eculizumab.A235000 Patients given eculizumab experienced less hemolysis caused by the membrane attack complex, but were still somewhat susceptible to hemolysis caused by C3b opsonization.A235000,A235005 Pegcetacoplan was developed out of a need for an inhibitor of complement mediated hemolysis further upstream of C5.A235000,A235005 Pegcetacoplan is a pegylated C3 inhibitor that can disrupt the processes leading to both forms of hemolysis that threaten patients with PNH.A235000

Pegcetacoplan for subcutaneous use was granted FDA approval on 14 May 2021.L34095 In February 2023, pegcetacoplan for intravitreal use was approved by the FDA for the treatment of geographic atrophy (GA) secondary to age-related macular degeneration.L45354

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The median half life in patients with PNH is 8.0 days.[L34095]
Volume Distribusi The volume of distribution in patients with PNH is 3.9 L.[L34095]
Klirens (Clearance) The mean clearance in patients with PNH is 0.37 L/day.[L34095]

Absorpsi

Pegcetacoplan has a median Tmax of 4.5-6.0 days.L34095 Patients reach steady state pharmacokinetics after 6-8 weeks.A235000

Metabolisme

Pegcetacoplan is expected to be metabolized to smaller oligopeptides and amino acids.L34095

Rute Eliminasi

Studies done in cynomolgus monkeys given radiolabeled pegcetacoplan suggest that the labelled peptide moiety is mainly excreted through urine. The elimination of PEG was not evaluated; however, it is known that it undergoes renal excretion.L44371

Interaksi Obat

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

Target Protein

Complement C3 C3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 33804461
    Fattizzo B, Serpenti F, Giannotta JA, Barcellini W: Difficult Cases of Paroxysmal Nocturnal Hemoglobinuria: Diagnosis and Therapeutic Novelties. J Clin Med. 2021 Mar 1;10(5). pii: jcm10050948. doi: 10.3390/jcm10050948.
  • PMID: 30135690
    Dobo J, Kocsis A, Gal P: Be on Target: Strategies of Targeting Alternative and Lectin Pathway Components in Complement-Mediated Diseases. Front Immunol. 2018 Aug 8;9:1851. doi: 10.3389/fimmu.2018.01851. eCollection 2018.
  • PMID: 10571018
    Tomita M: Biochemical background of paroxysmal nocturnal hemoglobinuria. Biochim Biophys Acta. 1999 Oct 8;1455(2-3):269-86. doi: 10.1016/s0925-4439(99)00068-x.
  • PMID: 24474777
    Baudino L, Sardini A, Ruseva MM, Fossati-Jimack L, Cook HT, Scott D, Simpson E, Botto M: C3 opsonization regulates endocytic handling of apoptotic cells resulting in enhanced T-cell responses to cargo-derived antigens. Proc Natl Acad Sci U S A. 2014 Jan 28;111(4):1503-8. doi: 10.1073/pnas.1316877111. Epub 2014 Jan 13.
  • PMID: 33464651
    de Castro C, Grossi F, Weitz IC, Maciejewski J, Sharma V, Roman E, Brodsky RA, Tan L, Di Casoli C, El Mehdi D, Deschatelets P, Francois C: C3 inhibition with pegcetacoplan in subjects with paroxysmal nocturnal hemoglobinuria treated with eculizumab. Am J Hematol. 2020 Nov;95(11):1334-1343. doi: 10.1002/ajh.25960. Epub 2020 Sep 11.
  • PMID: 33730455
    Hillmen P, Szer J, Weitz I, Roth A, Hochsmann B, Panse J, Usuki K, Griffin M, Kiladjian JJ, de Castro C, Nishimori H, Tan L, Hamdani M, Deschatelets P, Francois C, Grossi F, Ajayi T, Risitano A, de la Tour RP: Pegcetacoplan versus Eculizumab in Paroxysmal Nocturnal Hemoglobinuria. N Engl J Med. 2021 Mar 18;384(11):1028-1037. doi: 10.1056/NEJMoa2029073.

Contoh Produk & Brand

Produk: 6 • International brands: 1
Produk
  • Aspaveli
    Injection, solution • 1080 mg • Subcutaneous • EU • Approved
  • Aspaveli
    Injection, solution • 1080 mg • Subcutaneous • EU • Approved
  • Empaveli
    Injection, solution • 1080 mg/20mL • Subcutaneous • US • Approved
  • Empaveli
    Injection, solution • 1080 mg/20mL • Subcutaneous • US • Approved
  • Empaveli
    Solution • 1080 mg / 20 mL • Subcutaneous • Canada • Approved
  • Syfovre
    Injection, solution • 15 mg/0.1mL • Intravitreal • US • Approved
International Brands
  • Empaveli — Apellis Pharmaceuticals, Inc.

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