Darolutamide

Darolutamide Brand Name– NUBEQA

What is Darolutamide

Darolutamide is an androgen receptor inhibitor. It works by competitively inhibiting androgen binding to androgen receptors, thus inhibiting nuclear translocation of androgen receptors and their interaction with DNA.

It is indicated for the treatment of patients with nonmetastatic castration-resistant prostate cancer, where it significantly prolonged metastasis-free survival; overall survival data were not mature at the time of FDA approval.

Darolutamide differs from other FDA-approved androgen receptor inhibitors (e.g., apalutamide, enzalutamide) in that it has a distinct structure with fewer side effects, thought to be due to low penetration of the blood-brain barrier and low binding affinity for gamma-aminobutyric acid type A receptors.

Indications

  • prostate cancer

For the treatment of prostate cancer

for the treatment of nonmetastatic castration-resistant prostate cancer

Side Effects

  1. anemia
  2. anemia
  3. asthenia
  4. diarrhea
  5. elevated hepatic enzymes
  6. elevated hepatic enzymes
  7. erythema
  8. fatigue
  9. fatigue
  10. heart failure
  11. heart failure
  12. hot flashes
  13. hyperbilirubinemia
  14. hyperbilirubinemia
  15. hypertension
  16. hypertension
  17. lethargy
  18. maculopapular rash
  19. malaise
  20. musculoskeletal pain
  21. nausea
  22. nausea
  23. neutropenia
  24. neutropenia
  25. rash
  26. rash
  27. weight loss

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • breast-feeding
  • contraception requirements
  • females
  • hepatic disease
  • infertility
  • male-mediated teratogenicity
  • pregnancy
  • renal disease
  • renal failure
  • reproductive risk

Interactions

  • Abacavir; Dolutegravir; Lamivudine
  • Alpelisib
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Apalutamide
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Bictegravir; Emtricitabine; Tenofovir Alafenamide
  • Carbamazepine
  • Clarithromycin
  • Cobicistat
  • Conivaptan
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Dolutegravir
  • Dolutegravir; Lamivudine
  • Dolutegravir; Rilpivirine
  • Doravirine; Lamivudine; Tenofovir disoproxil fumarate
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Emtricitabine; Rilpivirine; Tenofovir alafenamide
  • Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
  • Emtricitabine; Tenofovir alafenamide
  • Emtricitabine; Tenofovir disoproxil fumarate
  • Fosphenytoin
  • Glecaprevir; Pibrentasvir
  • Glyburide
  • Glyburide; Metformin
  • grapefruit juice
  • Irinotecan
  • Irinotecan Liposomal
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ketoconazole
  • Lamivudine; Tenofovir Disoproxil Fumarate
  • Lopinavir; Ritonavir
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Methotrexate
  • Mifepristone
  • Nelfinavir
  • Ombitasvir; Paritaprevir; Ritonavir
  • Pazopanib
  • Phenobarbital
  • Phenytoin
  • Posaconazole
  • Prazosin
  • Primidone
  • Rifampin
  • Rimegepant
  • Ritonavir
  • Rosuvastatin
  • Saquinavir
  • St. John’s Wort, Hypericum perforatum
  • Sulfasalazine
  • Talazoparib
  • Telithromycin
  • Tenofovir Alafenamide
  • Tenofovir Alafenamide
  • Tenofovir, PMPA
  • Topotecan
  • Ubrogepant
  • Vemurafenib
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