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Aflibercept is a recombinant fusion protein that acts as a soluble decoy receptor for vascular endothelial growth factor (VEGF), a key regulator of angiogenesis. It binds to all isoforms of VEGF-A as well as VEGF-B and placental growth factor, and, thus, prevents them from binding to and activating their cognate receptors. In the USA and EU, intravenously administered aflibercept in combination with...
The prevalence of non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) is increasing world-wide in parallel to the increase of the obesity epidemic. Insulin resistance (IR) and the accumulation of triglyceride-derived toxic lipid metabolites play a key role in its pathogenesis. Multiple biomarkers are being evaluated for the non-invasive diagnosis of NASH. However, a...
Nebivolol is a highly selective β1-adrenergic receptor antagonist with a pharmacologic profile that differs from those of other drugs in its class. In addition to cardioselectivity mediated via β1 receptor blockade, nebivolol induces nitric oxide-mediated vasodilation by stimulating endothelial nitric oxide synthase via β3 agonism. This vasodilatory mechanism is distinct from those of other vasodilatory...
Apremilast (Otezla®) is an oral phosphodiesterase 4 inhibitor indicated for the twice-daily treatment of adults with psoriasis and psoriatic arthritis (PsA). Its use in these patient populations has been assessed in two phase III clinical trial programmes (ESTEEM and PALACE). At 16 weeks in the two ESTEEM trials, apremilast reduced the severity and extent of moderate to severe plaque psoriasis, including...
Imatinib is strongly positioned as the recommended first-line agent for most patients with advanced gastrointestinal stromal tumor (GIST) due to its good efficacy and tolerability. Imatinib-resistant advanced GIST continues to pose a therapeutic challenge, likely due to the frequent presence of multiple mutations that confer drug resistance. Sunitinib and regorafenib are approved as second- and third-line...
Collagenase Clostridium Histolyticum (CCH) (Xiaflex®, Xiapex®) intralesional injection is a mixture of class I (AUX-I) and class II (AUX-II) clostridial collagenases. It is indicated for the treatment of adult men with Peyronie’s disease with a palpable plaque and curvature deformity of ≥30° at the start of therapy. This article reviews the efficacy and tolerability of CCH in this indication and briefly...
Cangrelor (Kengrexal®, Kengreal™) is an intravenously administered P2Y12 receptor inhibitor. It is direct-acting and reversible, with a very rapid onset and offset of action. The randomized, double-blind, multinational, phase III CHAMPION PHOENIX trial compared the efficacy of intravenous cangrelor with that of oral clopidogrel in patients requiring percutaneous coronary intervention (PCI) for stable...
Endocrine therapy is a key component of adjuvant treatment for premenopausal patients with endocrine-responsive tumors. It is commonly well tolerated, although side effects are a main concern in the selection of treatment options. Tamoxifen is still considered an adequate endocrine therapy in a large group of premenopausal patients (e.g. lower-risk patient, presence of co-morbidities, patient preference)...
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) such as gefitinib, erlotinib, and afatinib are standard-of-care for first-line treatment of EGFR-mutant advanced non-small cell lung cancer (NSCLC). These drugs have a proven benefit in terms of higher response rate, delaying progression and improvement of quality of life over palliative platinum-based chemotherapy. The most...
An improved understanding of cancer genetics and immune regulatory pathways, including those associated with evasion of immune surveillance by tumours, has culminated in the development of several targeted therapies. One such strategy that acts to negate evasion of immune surveillance by tumours is inhibition of the programmed cell death receptor-1 (PD-1) checkpoint pathway. Intravenous nivolumab...
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