ENPNewswire-August 22, 2019--Ra Pharmaceuticals Earns Clinical Development Milestone for Oral Macrocyclic
Peptide Candidate Targeting Cardiovascular Indication Under Agreement with Merck
(NYSE:MRK) following the dosing of the first patient in a Phase 1 trial evaluating an investigational orally-available macrocyclic
peptide for a non-complement cardiovascular target.
Gadavist, also known as Gadovist and Gadovist 1.0 in other regions, is the US brand name of the aqueous 1.0M solution of gadobutrol, a gadolinium (Gd)-based extracellular contrast agent for MRI with a macrocyclic
structure, disclosed the company.
Initially, Nimble Therapeutics will leverage the speed and flexibility of its proprietary chemical synthesis platform, developed at Roche, to accelerate the discovery and optimization of macrocyclic
peptidomimetics as novel therapeutics.
According to their chemical structure, Gd-based contrast agents are subdivided into ionic and nonionic, macrocyclic
and linear contrast agents (see Table 1).
(40) There are two structural classes of Gd chelate complexes: macrocyclic
lactones (ML) are the most widely used deparasitizing treatment in cattle for control of endo--and ectoparasites (Rodriguez-Vivas et al., 2010; Davey, Pound, Miller, & Klavons, 2010).
The majority of the OPs, N-methyl carbamates, neonicotinoids, insect growth regulators, urea growth regulators, macrocyclic
lactones, synergists, and organosulfites were registered for agricultural uses during the study.
Firdaus, Template synthesis and spectroscopic characterization of 16-membered [N4] Schiff-base macrocyclic
complexes of Co(II), Ni(II), Cu(II), and Zn(II): in vitro DNA-binding studies, J.
Within the collaboration, Cyclenium will perform synthetic and medicinal chemistry activities to generate and optimize new macrocyclic
molecules effective against specific anti- infective targets chosen by AiCuris.
The need to evaluate alternative approaches is emphasized by the evolving susceptibility of Dirofilaria immitis larvae to heartworm preventatives containing macrocyclic
lactones, such as ivermectin.