Macitentan is a novel dual ETA/ETB receptor antagonist with enhanced tissue distribution and sustained receptor binding properties designed to achieve a more efficacious ET receptor blockade.
Taken together, the stronger IGABA enhancement by SCT-66 was accompanied by an apparent change in receptor subtype dependence (SCT-66 was e.g. equally efficacious on receptors comprising different β-subunits compared to piperine that was more efficacious on β2/3 incorporating receptors, compare Fig. 2B to Fig. 2E).
Varenicline, a partial agonist at the α4β2 nicotinic acetylcholine receptor, is more efficacious for smoking cessation than placebo and bupropion, and at least equally efficacious as nicotine replacement products.
In a series of comparative studies, azilsartan medoxomil as a single agent was found to be more efficacious than other widely used angiotensin receptor blockers at their maximum approved doses 19,20.
Subgroup analysis showed receptor fusion proteins were more efficacious for uveitis than placebo (OR: 0.30, 95% CI: 0.09 0.94, P = 0.04), but monoclonal antibodies were not (OR: 0.43, 95% CI: 0.12 1.49, P = 0.18).
Compared to the bispecific/divalent diabody, the tetravalent di-diabody binds more efficiently to both of its target antigens and is more efficacious in blocking ligand binding to the receptors.
However, Subgroup analysis showed the receptor fusion protein ETA was more efficacious than placebo for uveitis in this patient population, whereas monoclonal anti-TNF antibodies were not.
Both SNC80 and ARM390 produced similar levels of receptor stimulation, while Met-enkephalin was slightly more efficacious.
A full, more efficacious agonist would only need to occupy only a few receptors in order to elicit a response, and thus the EC50 value will be lower than the KD value.
For example, the price of medication impacts on its efficacy, with more expensive medications being more efficacious than cheaper ones.
