Bosentan - CAS 147536-97-8
Catalog number: 147536-97-8
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Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary artery hypertension (PAH). It is used as a vasodilator.
> 95%
Pale Yellow to Off-White Solid
4-(1,1-Dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2’-bipyrimidin]-4-yl]benzenesulfonamide; p-tert-Butyl-N-[6-(2-hydroxyethoxy)-5-(o-methoxyphenoxy) -2-(2-pyrimidinyl)-4-pyrimidinyl]benzenesulfonamide; Actelion; Ro 47-0203; Ro 47-0203/039; Tra
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1. Mutual pharmacokinetic interactions between steady-state bosentan and sildenafil
Gary Burgess & Hans Hoogkamer & Lorraine Collings & Jasper Dingemanse. Eur J Clin Pharmacol (2008) 64:43–50
As physicians try to optimise clinical efficacy to treat PAH, they may prescribe combination therapies with complementary mechanisms of action. Results from preliminary reports on treating patients with PAH with a combination of sildenafil and bosentan are encouraging. However, before such treatment is used widely, it is important for potential pharmacokinetic interactions to be understood and evaluated for interactions between the medications. Bosentan is a substrate and a known inducer of cytochromes P450-3A4 (CYP3A4) and CYP2C9. As sildenafil is predominantly metabolised by CYP3A4 and CYP2C9, there is a potential for a pharmacokinetic interaction between bosentan and sildenafil. Indeed, in a preliminary study, bosentan decreased the plasma concentrations of sildenafil when the two drugs were co-administered to patients with PAH.
2. Initial experience with bosentan (Tracleer®) as treatment for pulmonary arterial hypertension (PAH) due to congenital heart disease in infants and young children
N. Gilbert, Y.-C. Luther, O. Miera. Z Kardiol 94:570–574 (2005)
Follow-up of bosentan treatment was 4–18 months (mean 8.6 months). There was a reduction of right ventricular systolic pressure to 72±26 mmHg (p<0.05) (see Fig. 1); in those children who had received a banding, the RVSP decreased further from 92±11 to 47±11 mmHg. This was associated with an improvement of clinical status (reduction of NYHA class from 2.6±0.6 to 1.7±0.6, p<0.05) (see Fig. 2). One patient showed an increase of liver enzymes to almost three times the normal upper limit so that the usual doubling of the bosentan dose was delayed accordingly. Otherwise bosentan therapy was well tolerated in all patients without signs of discomfort or significant laboratory changes. There was no change in the transcutaneous oxygen saturation. Two patients died of cardiac decompensation, patient 1 due to severe pneumonia at the age of 21 months and patient 2 following an epileptic seizure at the age of 15 months (see Table 1).
3. N-Terminal probrain natriuretic peptide as a biochemical marker in the evaluation of bosentan treatment in systemic-sclerosis-related pulmonary arterial hypertension
Theodoros Dimitroulas & Georgios Giannakoulas &Haralambos Karvounis & Georgios Koliakos. Clin Rheumatol (2008) 27:655–658
Our study evaluated the effect of first-line bosentan treatment on NT-proBNP and SMWT in SScPAH. We found a statistically significant decrease of NT-proBNP values in the patients of our study after 20 weeks of bosentan treatment. To the best of our knowledge, there are no data evaluating the role of NT-proBNP, as a follow-up biochemical marker in SScPAH patients under bosentan treatment. Our results are in line with those of a recent study, which showed significant decrease in NT-proBNP levels in patients with IPH, after 20 weeks of bosentan treatment.
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Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary artery hypertension (PAH). It is used as a vasodilator.

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