From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

Boss, Christoph; Bolli, Martin H.; Gatfield, John

doi:10.1016/j.bmcl.2016.06.014

Cited by 22 publications

(14 citation statements)

References 96 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Bosentan and Macitentan, dual receptor antagonists; Ambrisentan, a selective ET A receptor antagonist; All used for the treatment of pulmonary hypertension [175].…”

Section: Calcitonin (Ct) Receptormentioning

confidence: 99%

Neuropeptide signalling systems – An underexplored target for venom drug discovery

Mendel

Kaas

Muttenthaler

2020

Biochemical Pharmacology

View full text Add to dashboard Cite

“…Bosentan and Macitentan, dual receptor antagonists; Ambrisentan, a selective ET A receptor antagonist; All used for the treatment of pulmonary hypertension [175].…”

Section: Calcitonin (Ct) Receptormentioning

confidence: 99%

Neuropeptide signalling systems – An underexplored target for venom drug discovery

Mendel

Kaas

Muttenthaler

2020

Biochemical Pharmacology

View full text Add to dashboard Cite

“…In addition to its vasoconstricting properties, ET-1 has also been shown to stimulate fibroblast and smooth muscle proliferation, which are key features of the underlying vasculopathy seen in scleroderma [22]. ET-1 accomplishes cell signaling through two receptors, ET A and ET B [46,47]. ET A and ET B are expressed on vascular smooth muscle cells; activation of these receptors by ET-1 mediates vasoconstriction.…”

Section: Pharmacologic Treatment: Systemic Therapymentioning

confidence: 99%

Pharmacotherapy Options in the Management of Raynaud’s Phenomenon

Hinze

Wigley

2018

Curr Treat Options in Rheum

View full text Add to dashboard Cite

Purpose of review: Multiple classes of medications have been studied for the treatment of Raynaud’s phenomenon (RP) with or without digital ischemia. The goal of this review is to discuss the outcomes of recent studies and to report on our approach to the management of RP in light of the available evidence. Recent findings: Comparing treatments for RP remains a challenge as efficacy endpoint vary widely among trials. While calcium channel blockers are used first-line in the pharmacologic management of RP, phosphodiesterase 5 inhibitors have also been shown to be beneficial in reducing symptoms. In the setting of digital ischemia, administration of intravenous prostanoids is the standard of care. Bosentan has shown benefit in the prevention of future ulcers in patients with scleroderma. Botulinum toxin therapy was ineffective in a clinical trial involving scleroderma patients; more controlled studies are needed in other subsets of patients. Digital sympathectomy may be beneficial in cases of critical digital ischemia, though recurrence of symptoms is common. Summary: Comparative effectiveness studies are needed to determine which therapeutic interventions are most beneficial in patients with RP. Based on the available evidence, we start with CCBs and add a phosphodiesterase inhibitor if symptoms are not controlled, or intravenous prostacyclin in the setting of severe critical digital ischemia. We may additionally add an endothelial receptor antagonist in cases of recurrent digital ulcers. A surgical sympathectomy may be used in refractory cases of digital ischemia. A digital block may also be a less invasive, but temporary, intervention allowing for titration of medical therapy.

show abstract

Section: Specific Managementmentioning

confidence: 99%

“…Both ET A and ET B receptors facilitate vasoconstriction and proliferation of vascular smooth muscle cells. In addition to expression in vascular smooth muscle cells, ET B is also found in endothelial cells, fibroblasts, and neuronal cells [Boss et al 2016]. ET B has a dual role and mediates vasodilation via NO, as well as facilitate the clearance of endothelin [Giaid et al 1993; Benigni and Remuzzi, 1999].…”

Section: Specific Managementmentioning

confidence: 99%

A review of therapeutic agents for the management of pulmonary arterial hypertension

Hahn

Makaryus

Talwar

et al. 2016

Ther Adv Respir Dis

View full text Add to dashboard Cite

Pulmonary arterial hypertension (PAH) is an uncommon, progressive and life threatening disease characterized by a proliferative vasculopathy of the small muscular pulmonary arterioles resulting in elevated pulmonary vascular resistance and eventually right ventricular failure. An increasing understanding of the pathobiology of PAH and its natural history has led to the development of numerous targeted therapies. Despite these advances there is significant progression of disease and the survival rate remains low. This article reviews the agents currently available for the medical management of PAH.

show abstract

From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

Cited by 22 publications

References 96 publications

Neuropeptide signalling systems – An underexplored target for venom drug discovery

Neuropeptide signalling systems – An underexplored target for venom drug discovery

Pharmacotherapy Options in the Management of Raynaud’s Phenomenon

A review of therapeutic agents for the management of pulmonary arterial hypertension

Contact Info

Product

Resources

About