- |||||||||| Journal: Recent advances in the diagnosis and therapy of large vessel vasculitis. (Pubmed Central) - Jul 2, 2022
On the other hand, tocilizumab may be used to treat both diseases. Promising targeted therapies evaluated in ongoing clinical trials include, for example, anti-IL-12/23 (ustekinumab), anti-IL-17 (secukinumab), anti-IL-1 (anakinra), anti-IL-23 (guselkumab), anti-cytotoxic T-lymphocyte antigen 4 (abatacept), Janus kinase inhibitors (tofacitinib and upadacitinib), anti-granulocyte / macrophage colony-stimulating factor (mavrilimumab), and endothelin receptor (bosentan) therapies.
- |||||||||| Zontivity (vorapaxar) / Merck (MSD), Tracleer (bosentan) / J&J, Roche
Review, Journal: Review new concepts in pharmacotherapy for peripheral arterial disease. (Pubmed Central) - Jun 29, 2022
Personalized management, identification of risk factors and shared-decision making are crucial in improving the best medical therapy for patients with PAD. Further studies are needed to assess the long-term safety and efficacy of novel strategies in real-world patients.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Preclinical, Journal: Different cardiovascular and pulmonary phenotypes for single- and double-knock-out mice deficient in BMP9 and BMP10. (Pubmed Central) - Jun 25, 2022
Our data show redundant roles for BMP9 and BMP10 in cardiovascular homeostasis under normoxic conditions (only combined deletion of both Bmp9 and Bmp10 was associated with severe defects) but highlight specific roles under chronic hypoxic conditions. We obtained evidence that BMP9 contributes to chronic hypoxia-induced pulmonary vascular remodelling, whereas BMP10 plays a role in hypoxia-induced cardiac remodelling in mice.
- |||||||||| Ventavis (iloprost) / Bayer, J&J, University of Copenhagen, Tracleer (bosentan) / J&J, Roche
Journal: Adenosine reverses life-threatening persistent pulmonary hypertension of the neonate refractory to triple vasodilator therapy. (Pubmed Central) - Jun 22, 2022
Persistent pulmonary hypertension of the neonate can cause acute and life-threatening hypoxia, but preterm neonates are not suitable candidate to extra-corporeal life support. We report the unique case of an extremely preterm neonates with life-threatening persistent pulmonary hypertension refractory to triple vasodilator therapy (nitric oxide, iloprost, and bosentan), which has been successfully treated with the addition of adenosine continuous infusion.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Journal: Thinking of bosentan repurposing - A study on dehydration and amorphization. (Pubmed Central) - Jun 22, 2022
Yet, the amorphous form recrystallized into the monohydrate form in the gastric milieu. This phenomenon was accompanied by a reversible color change from yellow, which is typical of bosentan glass, to creamywhite that is characteristic of the crude crystalline drug.
- |||||||||| Opsumit (macitentan) / Nippon Shinyaku, J&J, Tracleer (bosentan) / J&J, Roche
Behavior of right atrial strain in patients with advanced idiopathic pulmonary arterial hypertension after initiation of specific combined therapy (Research Gateway 7) - Jun 15, 2022 - Abstract #ESC2022ESC_5051;
RA peak longitudinal strain (PLS) and peak active contraction strain (PACS) were retrospectively assessed in 38 patients with advanced idiopathic pulmonary arterial hypertension (IPAH) who were referred to Aswan heart Centre and not receiving proper GDMT; at baseline and during follow-up after initiation of specific PAH combination therapy in the form of either Sildenafil/Bosentan or Sildenafil/Macitentan. Initiation of specific PAH combination therapy in undertreated patients with IPAH showed improvement in RA strain parameters despite no change in RA area during follow up.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Trial completion, Enrollment change, Trial completion date, Trial primary completion date: UMMC_Pilot: Vascular Dysfunction in Black Individuals: Roles of Nitric Oxide and Endothelin-1 (clinicaltrials.gov) - Jun 13, 2022
P1, N=8, Completed,
Selexipag, added as triple combination therapy in patients with PAH intermediate risk, improved risk variables, was well tolerated and achieved a medium-long- term free-event survival greater than 80%. Recruiting --> Completed | N=60 --> 8 | Trial completion date: May 2022 --> Sep 2021 | Trial primary completion date: May 2022 --> Sep 2021
- |||||||||| warfarin / Generic mfg.
Journal: Effects of concomitant administration of PXR ligand drugs on the anticoagulant effects of warfarin. (Pubmed Central) - Jun 8, 2022
However, switching from bosentan to macitentan resulted in a median of 2.25 reduction of the anticoagulant index rather than recovery of the response to warfarin. This study suggests not only the possibility of heterogeneity in the response to PXR activation and deactivation, but also the importance of long-term monitoring of drug-drug interactions when switching from bosentan to macitentan.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Clinical, Review, Journal: Nonsurgical treatment of cerebral ischemia associated with ACTA2 cerebral arteriopathy: a case report and literature review. (Pubmed Central) - Jun 4, 2022
After bosentan initiation, the patient's repetitive episodes of cerebral ischemia ceased, and there has been no increase in the number of white matter lesions for 7 years. Bosentan might be beneficial for treating cerebral ischemia associated with ACTA2 cerebral arteriopathy by maintaining the dilatation of stenotic vessels and adequate systemic blood flow and should be considered before performing revascularization surgery.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Bosentan? (Twitter) - May 27, 2022
- |||||||||| Tracleer (bosentan) / J&J, Roche
Journal: Dual Endothelin Receptor Antagonism Increases Resting Energy Expenditure in People with Increased Adiposity. (Pubmed Central) - May 20, 2022
Bosentan might be beneficial for treating cerebral ischemia associated with ACTA2 cerebral arteriopathy by maintaining the dilatation of stenotic vessels and adequate systemic blood flow and should be considered before performing revascularization surgery. Taken together, these results suggest that modulation of the endothelin system may represent a novel therapeutic approach to increase both resting metabolism and caloric expenditure, and reduce CVD risk in people with increased adiposity.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Journal: Comprehensive Update on Synthetic Aspects of Bosentan Derivatives. (Pubmed Central) - May 12, 2022
Bosentan synthesis has been reported by employing different methods from the reaction between (4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine and 4-(tert-butyl) benzenesulfonamide and 4-(tert-butyl)-N-(6-chloro-5-(2-methoxy phenoxy)-[2,2'-bipyrimidin]-4-yl) benzenesulfonamide in the form of different salt like potassium salt, ammonium salt ,sodium salt and isolated as free, on its reaction with ethylene glycol. Various modifications have been observed in the chemistry of the intermediates synthesis of the involved, particularly coupling chemistry to afford bosentan derivatives in high purity and yield.
- |||||||||| Tracleer (bosentan) / J&J, Roche, tadalafil / Generic mfg.
Tadalafil, Bosentan (Twitter) - May 9, 2022
- |||||||||| Ventavis (iloprost) / Bayer, J&J, University of Copenhagen, Botox (onabotulinumtoxin A) / GSK, AbbVie, Healis Therap, Tracleer (bosentan) / J&J, Roche
PDE5i, Bosentan or other Endothelin Ant Rc, NTG oilment, Botox, iloprost and sympathectomy (Twitter) - May 7, 2022
- |||||||||| sildenafil / Generic mfg., Ventavis (iloprost) / Bayer, J&J, University of Copenhagen, Tracleer (bosentan) / J&J, Roche
Iloprost Bosentan Sildenafil (Twitter) - May 7, 2022
- |||||||||| Tracleer (bosentan) / J&J, Roche
Clinical, PK/PD data, Journal: Population Pharmacokinetics of Tadalafil in Pediatric Patients with Pulmonary Arterial Hypertension: A Combined Adult/Pediatric Model. (Pubmed Central) - Apr 26, 2022
P1/2, P3
A one-compartment model parameterized in terms of F, absorption rate constant, CL/F, and V/F described the data well. The model demonstrated that plasma tadalafil concentrations in pediatric patients aged 2 to < 18 years were similar to those in adults at similar doses, and confirmed that dosing of 40 mg once daily in pediatric patients with a bodyweight ≥ 40 kg, and a dose of 20 mg once daily in patients with a body weight < 40 kg and aged ≥ 2 years are suitable for phase III evaluation.
- |||||||||| Adempas (riociguat) / Bayer, Tracleer (bosentan) / J&J, Roche
Review, Journal: Diagnosis and Treatment of Pulmonary Arterial Hypertension: A Review. (Pubmed Central) - Apr 19, 2022
Pulmonary arterial hypertension affects an estimated 10.6 per 1 million adults in the US and, without treatment, typically progresses to right heart failure and death. First-line therapy with drug combinations that target multiple biological pathways are associated with improved survival.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Trial completion date, Trial primary completion date: ENDOTHELION Study Group: Effect of Bosentan in NAION Patients (clinicaltrials.gov) - Apr 12, 2022
P3, N=86, Recruiting,
First-line therapy with drug combinations that target multiple biological pathways are associated with improved survival. Trial completion date: Aug 2020 --> Dec 2025 | Trial primary completion date: Dec 2019 --> Dec 2023
- |||||||||| Tracleer (bosentan) / J&J, Roche
Journal: Studies on the Vitrified and Cryomilled Bosentan. (Pubmed Central) - Mar 29, 2022
2011, 346, 1061-1064] for trehalose (TRE), was revealed on the basis of infrared and thermal measurements. Finally, two various hypotheses explaining water removal upon cryomilling have been discussed in the manuscript.
- |||||||||| Ventavis (iloprost) / Bayer, J&J, University of Copenhagen
Retrospective data, Journal: Management of Severe Scoliosis with Pulmonary Arterial Hypertension: A Single-Center Retrospective Case Series Study. (Pubmed Central) - Mar 25, 2022
The anesthetic management of scoliosis patients with PAH is important task that, like its own surgery, relies on the input of the multidisciplinary team for its success. Close monitoring, optimization of systemic blood pressure, pain control, oxygenation and ventilation, avoidance of exacerbating factors, and the use of vasopressors and pulmonary vasodilators when necessary are essential elements of management.
- |||||||||| Adempas (riociguat) / Bayer, Uptravi (selexipag) / J&J, Nippon Shinyaku, Tracleer (bosentan) / J&J, Roche
INOPERABLE CTEPH WITH DECOMPENSATED RIGHT HEART FAILURE AND AWAKE VA ECMO AS A BRIDGE TO TRANSPLANT ([VIRTUAL]) - Mar 23, 2022 - Abstract #SCCM2022SCCM_1295;
She was NYHA class III with 6-meter walk distance of 342 m. She had chronic corpulmonale on triple therapy with selexipag riociguat, bosentan, and warfarin...Milrinone and norepinephrine were started, and she was monitored with volume assessment, point of care ultrasound, NT proBNP and lactic acid...IV epoprostenol was initiated with discontinuation of selexipag...ECMO should be considered if the patient has been evaluated for transplant or has a realistic chance of receiving organs. Awake ECMO is preferred and is associated with better outcomes.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Biomarker, Journal: Network modeling predicts personalized gene expression and drug responses in valve myofibroblasts cultured with patient sera. (Pubmed Central) - Mar 15, 2022
Lastly, we performed virtual drug screening to identify patient-specific drug responses, which were experimentally validated via fibrotic gene expression measurements in valvular interstitial cells cultured with AVS patient sera and treated with or without bosentan-a clinically approved ET1 receptor inhibitor. In sum, our work advances the ability of computational approaches to provide a mechanistic basis for clinical decisions including patient stratification and personalized drug screening.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Journal: Cardioprotective effects of bosentan in 5-fluorouracil-induced cardiotoxicity. (Pubmed Central) - Feb 22, 2022
Bosentan had a significant cardioprotective effect against 5-FU induced cardiac damage. This effect may be attributed to its ability to inhibit endothelin receptors, stimulates eNOS, anti-oxidant, anti-inflammatory, anti-apoptotic properties with modulation of TLR4/MyD88/NFκB signaling pathway.
- |||||||||| Tracleer (bosentan) / J&J, Roche
Pulmonary Arterial Hypertension and Pregnancy at 2640 Meters Above Sea Level (Area K, Hall F (North Building, Exhibition Level), Moscone Center) - Feb 19, 2022 - Abstract #ATS2022ATS_4752;
We present a case where a multidisciplinary approach results in a good outcome.Case report: A 33-year-old woman with idiopathic pulmonary arterial hypertension (iPAH) diagnosed in 2018, treated with sildenafil 50 mg tid, bosentan 125 mg bid and treprostinil 38 ng/kg/min gets pregnant without desires of stop pregnancy...The periprocedural management included labetalol, diuretics and volume control to avoid overload and decompensation...The risk doesn’t end after birth, because a nearly follow up is necessary using de risk stratification tools.Conclusión: Maternal morbi-mortality is high in iPAH, so counseling is key. When it occurs, interruption of pregnancy is recommended but when this is not contemplated, management by a multidisciplinary group with specific therapy can help to have better outcomes.
- |||||||||| Mozobil (plerixafor) / Sanofi, Tracleer (bosentan) / J&J, Roche
MMP19 Mediates Pulmonary Fibrosis by Induction of Endothelial-to-Mesenchymal Transition (Room 212-214 (South Building, Level 2), Moscone Center) - Feb 19, 2022 - Abstract #ATS2022ATS_2109;
Drug therapy, effect as well as adverse effects, in children with pulmonary hypertension and born preterm needs to be further evaluated. Up-regulation of MMP19 in endothelial cells induced by lung injury promoted E(nd)MT and mediates bleomycin-induced lung injury and repair and fibrosis through the induction of ET1 and SDF1.
|
