Macitentan

Macitentan Brand Name– Opsumit

What is Macitentan

Macitentan is an oral endothelin receptor antagonist indicated for the treatment of adults with pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression.

During clinical trials, treatment with macitentan resulted in delayed progression of PAH (decline in exercise ability, worsening symptoms, or need for additional PAH medication) and reduced hospitalizations.

Compared to placebo, macitentan improved 6-minute walking distance and World Health Organization functional class and significantly reduced morbidity and mortality irrespective of whether patients had been previously treated for PAH or were treatment-naive.

Macitentan may cause embryo-fetal toxicity including birth defects and fetal death during pregnancy.

For all female patients, macitentan is only available through a special restricted distribution program called the Opsumit REMS Program. For female patients of reproductive potential, pregnancy testing is required before and routinely during macitentan therapy.

Male patients are not required to participate in the Opsumit REMS program. More information is available at www.opsumitrems.com

Indications

  • pulmonary hypertension

For the treatment of pulmonary hypertension (PAH, WHO Group 1) to delay disease progression

Side Effects

  1. anemia
  2. angioedema
  3. edema
  4. elevated hepatic enzymes
  5. fluid retention
  6. headache
  7. hepatic failure
  8. hepatotoxicity
  9. hypotension
  10. infection
  11. infertility
  12. influenza
  13. nasal congestion
  14. oligospermia
  15. pharyngitis
  16. pruritus
  17. rash
  18. teratogenesis

Monitoring Parameters

  • hemoglobin/hematocrit
  • LFTs
  • pregnancy testing

Contraindications

  • anemia
  • breast-feeding
  • contraception requirements
  • hepatic disease
  • infertility
  • pregnancy
  • pregnancy testing
  • pulmonary edema
  • reproductive risk
  • veno-occlusive disease (VOD)

Interactions

  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Atazanavir; Cobicistat
  • Boceprevir
  • Cariprazine
  • Ceritinib
  • Cobicistat
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Duloxetine
  • Elbasvir; Grazoprevir
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Enzalutamide
  • Indinavir
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ketoconazole
  • Lesinurad
  • Lesinurad; Allopurinol
  • Letermovir
  • Lopinavir; Ritonavir
  • Lumacaftor; Ivacaftor
  • Lurasidone
  • Nefazodone
  • Ombitasvir; Paritaprevir; Ritonavir
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifampin
  • Ritonavir
  • St. John’s Wort, Hypericum perforatum
  • Sympathomimetics
  • Telaprevir
  • Telithromycin
  • Telotristat Ethyl
  • Tipranavir
  • Tucatinib
  • Voriconazole