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3 results about "Intrinsic activity" patented technology
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Intrinsic activity (IA) and efficacy refer to the relative ability of a drug-receptor complex to produce a maximum functional response. This must be distinguished from the affinity, which is a measure of the ability of the drug to bind to its molecular target, and the EC₅₀, which is a measure of the potency of the drug and which is proportional to both efficacy and affinity. This use of the word "efficacy" was introduced by Stephenson (1956) to describe the way in which agonists vary in the response they produce, even when they occupy the same number of receptors. High efficacy agonists can produce the maximal response of the receptor system while occupying a relatively low proportion of the receptors in that system. There is a distinction between efficacy and intrinsic activity.
Bioavailability and bioequivalence through intrinsic activity and KD measurements, in vivo, in humans
Bioequivalence and / or bioavailability data are mandatory for filing of NDA and ANDA. Presently in absence of proper procedures estimates of these data through peak plasma level concentrations and time to reach peak plasma levels are used. The method suffers from the serious drawback that peak plasma levels do not correlate with efficacy due to delay in transfer to tissue sites as well as differences in metabolic patterns in drugs. Here we have devised a novel method for determination of bioavailability and bioequivalence from measurement of threshold times and concentrations, intrinsic activity, and dissociation constants in vivo in humans. The method essentially determines Intrinsic activities and threshold doses through measurement of drug responses in humans and then uses a mathematical expression to determine KD values of drugs, in vivo, in humans. The process may be applied to animals as well. The method would go a long way in evaluation of true bioavailability and bioequivalence and would also be useful in design.
Owner:BANERJEE DEBASISH
Methane-oxidizing bacterium for producing PHB and method for producing PHB by using methane-oxidizing bacterium
The present application relates to: a methane-oxidizing bacterium having an enhanced PHB-producing ability by having malate sulfur kinase activity higher than its intrinsic activity; a PHB production method comprising a step of culturing the methane-oxidizing bacteria in a culture medium; a PHB production composition comprising the methane-oxidizing bacterium, a culture of the methane-oxidizing bacterium, a fermentation product of the methane-oxidizing bacterium, or a combination of at least two thereof; the invention also discloses a PHB production application of the methane-oxidizing bacteria.
Owner:CJ CHEILJEDANG CORP
Interferon-induced transmembrane protein scaffold for engineering extracellular vesicles
PCT designated stageWO2026111414A1Polypeptide with localisation/targeting motifCell dissociation methodsExtracellular vesicleHigh level expression
The present invention relates to an IFITM scaffold enabling high-efficiency engineering of extracellular vesicles. In the present invention, active substances to be expressed in extracellular vesicles are linked to the IFITM scaffold so that the active substances can be expressed in the vesicles at a high level. In particular, the active substance linked to the C-terminus of the IFITM scaffold is present on the surface of the vesicles to exhibit the intrinsic activity. In addition, the present invention provides a U-shaped IFITM scaffold, which enables two types of active substances linked to the N-terminus and the C-terminus of the IFITM scaffold to be present on the surface of extracellular vesicles at a 1:1 ratio.
Owner:SHIFTBIO INC +1