Peringatan Keamanan

There are limited data on rozanolixizumab-noli use in pregnant women to inform a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Following the administration of rozanolixizumab-noli to pregnant monkeys at doses greater than those used clinically, increases in embryonic death, reduced body weight, and impaired immune function were observed in the absence of maternal toxicity.L47117

Subcutaneous administration of rozanolixizumab-noli (0 or 150 mg/kg) every 3 days for 26 weeks to sexually mature cynomolgus monkeys resulted in no adverse effects on sperm parameters (count, motility, or morphology) or estrus cyclicity. The dose tested in monkeys is 30 times the maximum recommended human dose of approximately 10 mg/kg, on a mg/kg/week basis.L47117

Rozanolixizumab

DB14919

biotech approved investigational

Deskripsi

Rozanolixizumab is a humanized high-affinity anti-human neonatal Fc receptor (FcRn) monoclonal antibody (IgG4P) targeting the immunoglobulin G (IgG). Rozonolixizumab itself is an IgG4P, an inactive isotype, to reduce the likelihood of unwanted chain exchange.A260177 It is investigated for use in autoimmune and alloimmune diseases with pathologic IgG, particularly generalized myasthenia gravis.A260182 Generalized myasthenia gravis is characterized by the formation of IgG antibodies against the nicotinic acetylcholine receptor (AChR) or muscle-specific tyrosine kinase (MuSK).A260187,A260192,A260197 Approximately 80% of myasthenia gravis patients tested positive for the AChR autoantibodies, and 40% of these AChR-negative or seronegative patients were found to have MuSK autoantibodies.A260207

AChR is vital for signal transduction in the neuromuscular junctions (NMJ) by generating muscle end plate potentials to propagate action potential.A260192 Therefore, the presence of AChR-antibodies can interfere with the ACh-mediated downstream signaling, thus reducing the likelihood of end plate potentials reaching the threshold needed to trigger an action potential.A260192 As a result, the main clinical manifestation of myasthenia gravis is easily fatigable or persistent muscle weakness.A260192 On the other hand, MuSK activation can trigger the clustering of AChR at the NMJ, guide the innervation of motor neurons toward AChR-dense areas, and anchor acetylcholinesterase.A260187,A260202 Therefore, autoantibodies against MuSK can also affect the signal propagation at the NMJ.

Rozanolixizumab-noli is available under the brand name RYSTIGGO and was developed by UCB.L47122 It was granted orphan drug designation by the FDA in 2019, by the European Medicines Agency (EMA) in April 2020, and by the Japanese Pharmaceuticals and Medical Devices Agency (PMDA) in November 2020.L47122 In June 2023, Rozanolixizumab-noli was approved by the FDA under Priority Review for the treatment of adult patients with generalized myasthenia gravis who are positive for the anti-acetylcholine receptor (AchR) or anti-muscle-specific tyrosine kinase (MuSK) antibody.L47122 This is due to the efficacy demonstrated in the pivotal Phase 3 MycarinG study (NCT03971422).L47122 Rozanolixizumab was also approved by the European Commission on January 5, 2024.L50973

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi The apparent volume of distribution of rozanolixizumab-noli is 6.6 L.[L47117]
Klirens (Clearance) The apparent clearance for the rozanolixizumab-noli is 0.89 L/day.[L47117]

Absorpsi

Rozanolixizumab-noli exhibited nonlinear pharmacokinetics. Rozanolixizumab-noli exposure increased in a greater than dose-proportional manner over a dose range from 1 mg/kg to 20 mg/kg (two times the maximum recommended dose) following subcutaneous administration.L47117 Following subcutaneous administration of rozanolixizumab-noli, peak plasma levels were achieved after approximately 2 days in healthy subjects.L47117

Metabolisme

Rozanolixizumab-noli is expected to be degraded by proteolytic enzymes into small peptides and amino acids.L47117

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

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

Target Protein

IgG receptor FcRn large subunit p51 FCGRT

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29093180
    Kiessling P, Lledo-Garcia R, Watanabe S, Langdon G, Tran D, Bari M, Christodoulou L, Jones E, Price G, Smith B, Brennan F, White I, Jolles S: The FcRn inhibitor rozanolixizumab reduces human serum IgG concentration: A randomized phase 1 study. Sci Transl Med. 2017 Nov 1;9(414):eaan1208. doi: 10.1126/scitranslmed.aan1208.
  • PMID: 30130439
    Smith B, Kiessling A, Lledo-Garcia R, Dixon KL, Christodoulou L, Catley MC, Atherfold P, D'Hooghe LE, Finney H, Greenslade K, Hailu H, Kevorkian L, Lightwood D, Meier C, Munro R, Qureshi O, Sarkar K, Shaw SP, Tewari R, Turner A, Tyson K, West S, Shaw S, Brennan FR: Generation and characterization of a high affinity anti-human FcRn antibody, rozanolixizumab, and the effects of different molecular formats on the reduction of plasma IgG concentration. MAbs. 2018 Oct;10(7):1111-1130. doi: 10.1080/19420862.2018.1505464. Epub 2018 Sep 12.
  • PMID: 29655451
    Rivner MH, Pasnoor M, Dimachkie MM, Barohn RJ, Mei L: Muscle-Specific Tyrosine Kinase and Myasthenia Gravis Owing to Other Antibodies. Neurol Clin. 2018 May;36(2):293-310. doi: 10.1016/j.ncl.2018.01.004.
  • PMID: 31998320
    Gable KL, Guptill JT: Antagonism of the Neonatal Fc Receptor as an Emerging Treatment for Myasthenia Gravis. Front Immunol. 2020 Jan 10;10:3052. doi: 10.3389/fimmu.2019.03052. eCollection 2019.
  • PMID: 32793097
    Rodolico C, Bonanno C, Toscano A, Vita G: MuSK-Associated Myasthenia Gravis: Clinical Features and Management. Front Neurol. 2020 Jul 23;11:660. doi: 10.3389/fneur.2020.00660. eCollection 2020.
  • PMID: 32982689
    Cao M, Koneczny I, Vincent A: Myasthenia Gravis With Antibodies Against Muscle Specific Kinase: An Update on Clinical Features, Pathophysiology and Treatment. Front Mol Neurosci. 2020 Sep 2;13:159. doi: 10.3389/fnmol.2020.00159. eCollection 2020.
  • PMID: 24297891
    Huijbers MG, Zhang W, Klooster R, Niks EH, Friese MB, Straasheijm KR, Thijssen PE, Vrolijk H, Plomp JJ, Vogels P, Losen M, Van der Maarel SM, Burden SJ, Verschuuren JJ: MuSK IgG4 autoantibodies cause myasthenia gravis by inhibiting binding between MuSK and Lrp4. Proc Natl Acad Sci U S A. 2013 Dec 17;110(51):20783-8. doi: 10.1073/pnas.1313944110. Epub 2013 Dec 2.

Contoh Produk & Brand

Produk: 5 • International brands: 0
Produk
  • Rystiggo
    Injection, solution • 140 mg/ml • Subcutaneous • EU • Approved
  • Rystiggo
    Injection, solution • 140 mg/1mL • Subcutaneous • US • Approved
  • Rystiggo
    Injection, solution • 140 mg/1mL • Subcutaneous • US • Approved
  • Rystiggo
    Injection, solution • 140 mg/1mL • Subcutaneous • US • Approved
  • Rystiggo
    Injection, solution • 140 mg/1mL • Subcutaneous • US • Approved

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