Peringatan Keamanan

In the event of an overdose of danicopan, increases in liver enzymes may occur. If an overdose is suspected, employ general supportive measures as clinically indicated.L50381

Danicopan

DB15401

small molecule approved investigational

Deskripsi

Paroxysmal nocturnal hemoglobinuria (PNH) is a rare acquired hematologic disease characterized by hemolysis, thrombophilia, and bone marrow dysfunction.A263501,L50417 Both hemolysis and thrombophilia are mediated primarily by the complement system.A263501 Standard therapy for PNH involves the use of complement C5 inhibitors (e.g. eculizumab, ravulizumab) which are effective in mitigating complement-mediated intravascular hemolysis and thromboembolism.A263501 Unfortunately, complement C5 inhibition does not address C3-mediated extravascular hemolysis, which occurs earlier in the complement cascade within the alternative pathway.A263501,L50411

Danicopan is a small molecule complement factor D inhibitor that selectively blocks the alternative pathway, thereby working to address extravascular hemolysis when used in conjunction with C5 inhibitors.L50381 It was first approved in January 2024 in Japan for patients with PNH,A263506,L50416 shortly after which the EMA adopted a positive opinion and recommended granting it marketing authorization.A263506 It was subsequently approved by the FDA in March 2024.L50386

Struktur Molekul 2D

Berat 580.418
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 half-life of danicopan is 7.9 hours.[L50381]
Volume Distribusi The apparent volume of distribution of danicopan for a 75 kg person was 395 liters.[L50381]
Klirens (Clearance) The mean apparent clearance of danicopan is 63 L/h.[L50381]

Absorpsi

The median Tmax is 3.7 hours following oral administration of 150 mg danicopan in patients with PNH.L50381 When administered with a high-fat meal, the AUC and Cmax of danicopan increase approximately 25% and 93%, respectively, compared to the fasted state. Median Tmax remains comparable whether administered fed or fasted.L50381

Metabolisme

Danicopan is extensively metabolized, primarily via oxidation, reduction, and hydrolysis pathways.L50381 The major pathway of elimination is amide hydrolysis. Although metabolism via CYP-mediated pathways is minimal, approximately 96% of danicopan is metabolized through the aforementioned non-CYP pathways.L50381 In vitro studies suggest that danicopan has a very low likelihood of being involved in CYP-based drug-drug interactions.L50381

Rute Eliminasi

Following the administration of a single radiolabeled dose of danicopan, 69% of total radioactivity was excreted in feces (3.57% as unchanged parent drug) and 25% was excreted in urine (0.48% as unchanged parent drug).L50381

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

522 Data
Folic acid The serum concentration of Folic acid can be increased when it is combined with Danicopan.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Danicopan.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Danicopan.
Gefitinib The serum concentration of Gefitinib can be increased when it is combined with Danicopan.
Allopurinol The serum concentration of Allopurinol can be increased when it is combined with Danicopan.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Danicopan.
Teniposide The serum concentration of Teniposide can be increased when it is combined with Danicopan.
Prazosin The serum concentration of Prazosin can be increased when it is combined with Danicopan.
Raloxifene The serum concentration of Raloxifene can be increased when it is combined with Danicopan.
Celecoxib The serum concentration of Celecoxib can be increased when it is combined with Danicopan.
Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Danicopan.
Ritonavir The serum concentration of Ritonavir can be increased when it is combined with Danicopan.
Oxaliplatin The serum concentration of Oxaliplatin can be increased when it is combined with Danicopan.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Danicopan.
Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Danicopan.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Danicopan.
Ivermectin The serum concentration of Ivermectin can be increased when it is combined with Danicopan.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Danicopan.
Testosterone The serum concentration of Testosterone can be increased when it is combined with Danicopan.
Clofarabine The serum concentration of Clofarabine can be increased when it is combined with Danicopan.
Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Danicopan.
Tamoxifen The serum concentration of Tamoxifen can be increased when it is combined with Danicopan.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Danicopan.
Daunorubicin The serum concentration of Daunorubicin can be increased when it is combined with Danicopan.
Nitrofurantoin The serum concentration of Nitrofurantoin can be increased when it is combined with Danicopan.
Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Danicopan.
Riluzole The serum concentration of Riluzole can be increased when it is combined with Danicopan.
Irinotecan The serum concentration of Irinotecan can be increased when it is combined with Danicopan.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Danicopan.
Sulfasalazine The serum concentration of Sulfasalazine can be increased when it is combined with Danicopan.
Donepezil The serum concentration of Donepezil can be increased when it is combined with Danicopan.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Danicopan.
Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Danicopan.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Danicopan.
Glyburide The serum concentration of Glyburide can be increased when it is combined with Danicopan.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Danicopan.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Danicopan.
Leflunomide The serum concentration of Leflunomide can be increased when it is combined with Danicopan.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Danicopan.
Mitoxantrone The serum concentration of Mitoxantrone can be increased when it is combined with Danicopan.
Dasatinib The serum concentration of Dasatinib can be increased when it is combined with Danicopan.
Prasterone The serum concentration of Prasterone can be increased when it is combined with Danicopan.
Alvocidib The serum concentration of Alvocidib can be increased when it is combined with Danicopan.
Camptothecin The serum concentration of Camptothecin can be increased when it is combined with Danicopan.
Nilotinib The serum concentration of Nilotinib can be increased when it is combined with Danicopan.
Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Danicopan.
Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Danicopan.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Danicopan.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Danicopan.
Pralatrexate The serum concentration of Pralatrexate can be increased when it is combined with Danicopan.
Teriflunomide The serum concentration of Teriflunomide can be increased when it is combined with Danicopan.
Vemurafenib The serum concentration of Vemurafenib can be increased when it is combined with Danicopan.
Ponatinib The serum concentration of Ponatinib can be increased when it is combined with Danicopan.
Dabrafenib The serum concentration of Dabrafenib can be increased when it is combined with Danicopan.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Danicopan.
Dolutegravir The serum concentration of Dolutegravir can be increased when it is combined with Danicopan.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Danicopan.
Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Danicopan.
Idelalisib The serum concentration of Idelalisib can be increased when it is combined with Danicopan.
Palbociclib The serum concentration of Palbociclib can be increased when it is combined with Danicopan.
Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Danicopan.
Fimasartan The serum concentration of Fimasartan can be increased when it is combined with Danicopan.
Ombitasvir The serum concentration of Ombitasvir can be increased when it is combined with Danicopan.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Danicopan.
Osimertinib The serum concentration of Osimertinib can be increased when it is combined with Danicopan.
Venetoclax The serum concentration of Venetoclax can be increased when it is combined with Danicopan.
Velpatasvir The serum concentration of Velpatasvir can be increased when it is combined with Danicopan.
Tucatinib The serum concentration of Tucatinib can be increased when it is combined with Danicopan.
Selumetinib The serum concentration of Selumetinib can be increased when it is combined with Danicopan.
Talazoparib The serum concentration of Talazoparib can be increased when it is combined with Danicopan.
Fostemsavir The serum concentration of Fostemsavir can be increased when it is combined with Danicopan.
Revefenacin The serum concentration of Revefenacin can be increased when it is combined with Danicopan.
Delafloxacin The serum concentration of Delafloxacin can be increased when it is combined with Danicopan.
Duvelisib The serum concentration of Duvelisib can be increased when it is combined with Danicopan.
Dacomitinib The serum concentration of Dacomitinib can be increased when it is combined with Danicopan.
Binimetinib The serum concentration of Binimetinib can be increased when it is combined with Danicopan.
Glasdegib The serum concentration of Glasdegib can be increased when it is combined with Danicopan.
Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Danicopan.
Alpelisib The serum concentration of Alpelisib can be increased when it is combined with Danicopan.
Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Danicopan.
Brigatinib The serum concentration of Brigatinib can be increased when it is combined with Danicopan.
Rucaparib The serum concentration of Rucaparib can be increased when it is combined with Danicopan.
Rimegepant The serum concentration of Rimegepant can be increased when it is combined with Danicopan.
Copanlisib The serum concentration of Copanlisib can be increased when it is combined with Danicopan.
Ozanimod Danicopan may decrease the excretion rate of Ozanimod which could result in a higher serum level.
Tazemetostat The serum concentration of Tazemetostat can be increased when it is combined with Danicopan.
Darolutamide The serum concentration of Darolutamide can be increased when it is combined with Danicopan.
Lusutrombopag The serum concentration of Lusutrombopag can be increased when it is combined with Danicopan.
Enasidenib The serum concentration of Enasidenib can be increased when it is combined with Danicopan.
Pibrentasvir The serum concentration of Pibrentasvir can be increased when it is combined with Danicopan.
Glecaprevir The serum concentration of Glecaprevir can be increased when it is combined with Danicopan.
Testosterone cypionate The serum concentration of Testosterone cypionate can be increased when it is combined with Danicopan.
Testosterone enanthate The serum concentration of Testosterone enanthate can be increased when it is combined with Danicopan.
Ripretinib The serum concentration of Ripretinib can be increased when it is combined with Danicopan.
Ubrogepant The serum concentration of Ubrogepant can be increased when it is combined with Danicopan.
Trilaciclib The serum concentration of Trilaciclib can be increased when it is combined with Danicopan.
Pralsetinib The serum concentration of Pralsetinib can be increased when it is combined with Danicopan.
Berotralstat The serum concentration of Berotralstat can be increased when it is combined with Danicopan.
Daptomycin The serum concentration of Daptomycin can be increased when it is combined with Danicopan.
Cyclosporine Danicopan may increase the immunosuppressive activities of Cyclosporine.

Target Protein

Complement factor D CFD

Referensi & Sumber

Synthesis reference: Wiles, JA et. al.; Achillion Pharmaceuticals Inc. "Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders." US Patent US20180179186A1. June 28, 2018.
Artikel (PubMed)
  • PMID: 33121236
    Risitano AM, Kulasekararaj AG, Lee JW, Maciejewski JP, Notaro R, Brodsky R, Huang M, Geffner M, Browett P: Danicopan: an oral complement factor D inhibitor for paroxysmal nocturnal hemoglobinuria. Haematologica. 2021 Dec 1;106(12):3188-3197. doi: 10.3324/haematol.2020.261826.
  • PMID: 38528310
    Kang C: Danicopan: First Approval. Drugs. 2024 Mar 26. doi: 10.1007/s40265-024-02023-6.

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