Macitentan: An important addition to the treatment of pulmonary arterial hypertension

Journal of Pharmacology and Pharmacotherapeutics

Volumn 6, Issue 1, 2015, Pages 53-57

  Khadka, Anjan ^a   Brashier, Dick B Singh ^a   Tejus, Anantharamu ^a   Sharma, Ashok Kumar ^a  

^a ARMED FORCES MEDICAL COLLEGE   (India)

Author keywords

Cancer; endothelin; macitentan; pulmonary arterial hypertension (PAH)

Indexed keywords

MACITENTAN;

ANEMIA; ANTIHYPERTENSIVE ACTIVITY; ANTINEOPLASTIC ACTIVITY; ARTICLE; BRONCHITIS; DRUG CONTRAINDICATION; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG INDICATION; DRUG INTERACTION; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SAFETY; EDEMA; HEADACHE; HUMAN; INFLUENZA; LIVER FAILURE; LIVER TOXICITY; MALE GENITAL SYSTEM DISEASE; MAXIMUM PLASMA CONCENTRATION; PHARYNGITIS; PHARYNX DISEASE; PHASE 3 CLINICAL TRIAL (TOPIC); PULMONARY HYPERTENSION; SPERMATOGENESIS; URINARY TRACT INFECTION;

EID: 84921972660     PISSN: 0976500X     EISSN: 09765018     Source Type: Journal    
DOI: 10.4103/0976-500X.149151     Document Type: Article

References (40)

1. Bruderer S, Hopfgartner G, Seiberling M, Wank J, Sidharta PN, Treiber A, et al. Absorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humans. Xenobiotica 2012; 42: 901-10
2. Lepist EI, Gillies H, Smith W, Hao J, Hubert C, St Claire RL, et al. Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes. PLoS One 2014; 9: e87548
3. Iglarz M, Binkert C, Morrison K, Fischli W, Gatfield J, Treiber A, et al. Pharmacology of macitentan, an orally active tissue-Targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther 2008; 327: 736-45
4. Sitbon O, Morrell N. Pathways in pulmonary arterial hypertension: The future is here. Eur Respir Rev 2012; 21: 321-7
5. Seferian A, Simonneau G. Therapies for pulmonary arterial hypertension: Where are we today, where do we go tomorrow? Eur Respir Rev 2013; 22: 217-26
6. Parida A, Nayak V. Endothelins: Their current status and future prospects. Int J Pharm Sci Rev Res 2013; 23: 94-7
7. Sidharta PN, van Giersbergen PL, Halabi A, Dingemanse J. Macitentan: Entry-into-humans study with a new endothelin receptor antagonist. Eur J Clin Pharmacol 2011; 67: 977-84
8. Wu Y, O'Callaghan DS, Humbert M. An update on medical therapy for pulmonary arterial hypertension. Curr Hypertens Rep 2013; 15: 614-22
9. Yao A. Recent advances and future perspectives in therapeutic strategies for pulmonary arterial hypertension. J Cardiol 2012; 60: 344-9
10. Pulido T, Rubin LJ, Simonneau G. Macitentan and pulmonary arterial hypertension. N Engl J Med 2014; 370: 82-3
11. Galiè N, Ghofrani AH. New horizons in pulmonary arterial hypertension therapies. Eur Respir Rev 2013; 22: 503-14
12. Bruderer S, Marjason J, Sidharta PN, Dingemanse J. Pharmacokinetics of macitentan in caucasian and Japanese subjects: The influence of ethnicity and sex. Pharmacology 2013; 91: 331-8
13. Humbert M, Souza R, Galiè N, McLaughlin V, Simonneau G, Rubin L. Pulmonary arterial hypertension: Bridging the present to the future. Eur Respir Rev 2012; 21: 267-70
14. Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, et al. The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl) oxy] ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem 2012; 55: 7849-61
15. Sidharta PN, van Giersbergen PL, Dingemanse J. Safety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple-dose study in healthy subjects. J Clin Pharmacol 2013; 53: 1131-8
16. Kim SJ, Kim JS, Kim SW, Yun SJ, He J, Brantley E, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol 2012; 5: 39-47
17. Kim SJ, Kim JS, Kim SW, Brantley E, Yun SJ, He J, et al. Macitentan (ACT-064992), a tissue-Targeting endothelin receptor antagonist, enhances therapeutic efficacy of paclitaxel by modulating survival pathways in orthotopic models of metastatic human ovarian cancer. Neoplasia 2011; 13: 167-79
18. Bruderer S, Aänismaa P, Homery MC, Häusler S, Landskroner K, Sidharta PN, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-Targeting dual endothelin receptor antagonist. AAPS J 2012; 14: 68-78
19. Gatfield J, Grandjean CM, Sasse T, Clozel M, Nayler O. Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells. PLoS One 2012; 7: e47662
20. Rosanò L, Spinella F, Bagnato A. The importance of endothelin axis in initiation, progression, and therapy of ovarian cancer. Am J Physiol Regul Integr Comp Physiol 2010; 299: R395-404
21. Spinella F, Rosanò L, Del Duca M, Di Castro V, Nicotra MR, Natali PG, et al. Endothelin-1 inhibits prolyl hydroxylase domain 2 to activate hypoxia-inducible factor-1alpha in melanoma cells. PLoS One 2010; 5: e11241
22. Knowles JP, Shi-Wen X, Haque SU, Bhalla A, Dashwood MR, Yang S, et al. Endothelin-1 stimulates colon cancer adjacent fibroblasts. Int J Cancer 2012; 130: 1264-72
23. Grant K, Loizidou M, Taylor I. Endothelin-1: A multifunctional molecule in cancer. Br J Cancer 2003; 88: 163-6
24. Kummer O, Haschke M, Hammann F, Bodmer M, Bruderer S, Regnault Y, et al. Comparison of the dissolution and pharmacokinetic profiles of two galenical formulations of the endothelin receptor antagonist macitentan. Eur J Pharm Sci 2009; 38: 384-8
25. Torbicki A, Mehta S, Perchenet L, Pulido T, Sastry BK, Sitbon O, et al. Effect of macitentan on haemodynamics in patients with pulmonary arterial hypertension: Results from the long-Term, randomised, placebo-controlled SERAPHIN trial. Eur Heart J 2013; 34(Suppl 1): 1062
26. Benza RL, Miller DP, Barst RJ, Badesch DB, Frost AE, McGoon MD. An evaluation of long-Term survival from time of diagnosis in pulmonary arterial hypertension from the REVEAL Registry. Chest 2012; 142: 448-56
27. Macchia A, Mariani J, Tognoni G. Macitentan and pulmonary arterial hypertension. N Engl J Med 2014; 370: 82
28. ThompsonCA. Macitentan approved by FDA to delay progression of PAH. Am J Health Syst Pharm 2013; 70: 2054
29. Patel T, McKeage K. Macitentan: First global approval. Drugs 2014; 74: 127-33
30. Raja SG. Macitentan, a tissue-Targeting endothelin receptor antagonist for the potential oral treatment of pulmonary arterial hypertension and idiopathic pulmonary fibrosis. Curr Opin Investig Drugs 2010; 11: 1066-73
31. Tonelli AR, Dweik RA. Macitentan and pulmonary arterial hypertension. N Engl J Med 2014; 370: 81-2
32. Weber MA, Black H, Bakris G, Krum H, Linas S, Weiss R, et al. A selective endothelin-receptor antagonist to reduce blood pressure in patients with treatment-resistant hypertension: A randomised, double-blind, placebo-controlled trial. Lancet 2009; 374: 1423-31
33. Raghu G, Million-Rousseau R, Morganti A, Perchenet L, Behr J. MUSIC Study Group. Macitentan for the treatment of idiopathic pulmonary fibrosis: The randomised controlled MUSIC trial. Eur Respir J 2013; 42: 1622-32
34. Sen S, Chen S, Feng B, Iglarz M, Chakrabarti S. Renal, retinal and cardiac changes in type 2 diabetes are attenuated by macitentan, a dual endothelin receptor antagonist. Life Sci 2012; 91: 658-68
35. Mule M, Scarabelli M, Capodanno D, Ussia GP, Tamburino C. Clinical pharmacotherapy and drug development for pulmonary arterial hypertension. Recent Pat Cardiovasc Drug Discov 2011; 6: 180-8
36. Weiss J, Theile D, Rüppell MA, Speck T, Spalwisz A, Haefeli WE. Interaction profile of macitentan, a new non-selective endothelin-1 receptor antagonist, in vitro. Eur J Pharmacol 2013; 701: 168-75
37. Kohan DE, Cleland JG, Rubin LJ, Theodorescu D, Barton M. Clinical trials with endothelin receptor antagonists: What went wrong and where can we improve? Life Sci 2012; 91: 528-39
38. Aubert JD, Juillerat-Jeanneret L. Therapeutic potential of endothelin receptor modulators: Lessons from human clinical trials. Expert Opin Ther Targets 2009; 13: 1069-84
39. Pulido T, Adzerikho I, Channick RN, Delcroix M, Galiè N, Ghofrani HA, et al. SERAPHIN Investigators. Macitentan and morbidity and mortality in pulmonary arterial hypertension. N Engl J Med 2013; 369: 809-18
40. Smith KA, Fraidenburg DR, Yuan JXJ. Targeted therapies: Endothelin receptor antagonists. In: Smith KA, Fraidenburg DR, Yuan JXJ, editors. Advances in the Management of Pulmonary Arterial Hypertension. London: Future Medicine Ltd; 2013. p. 64-73