Date: 2017-05-10
Type of
information: Presentation of results at a congress
phase: preclinical
Announcement: presentation of results at the Association for Research in Vision and Ophthalmology (ARVO)
Company: Cempra (USA - NC)
Product: ophthalmic solithromycin
Action
mechanism:
- antibiotic/macrolide. Solithromycin is a next-generation oral and intravenous fluoroketolide now in Phase 3 clinical development for the treatment of moderate to moderately-severe community acquired bacterial pneumonia (CABP) and urethritis. In vitro and in vivo studies have shown potent activity against S. pneumoniae as well as an extended spectrum of activity against CA-MRSA, enterococci, Mycobacterium avium and in animal models of malaria. It is also active against atypical bacteria, such as Legionella, Chlamydophila, Chlamydia, Mycoplasma and Ureaplasma and against gonococci and other organisms that cause genitourinary tract infections. It is 8-16 times more potent than azithromycin and is active against azithromycin-resistant strains. Its activity against resistant strains is driven by its ability to bind to three sites on the bacterial ribosome, compared to one or two for current macrolides. The binding to three ribosomal sites is expected to limit resistance development.
- Solithromycin does not contain a pyridine in the side chain of the molecule (as does telithromycin or Ketek®) that appears to interact with nicotinic acetylcholine receptors and could be associated with serious adverse events such as visual disturbances and exacerbations of myasthenia gravis that have been observed with telithromycin.
Disease:
Therapeutic
area: Infectious diseases
Country:
Trial
details:
Latest
news:
- • On May 10, 2017, Cempra announced that the company is presenting two abstracts highlighting topical ophthalmic formulations of solithromycin in preclinical models of activity, tolerability and pharmacokinetics (PK) in the eye at the annual meeting of the Association for Research in Vision and Ophthalmology (ARVO) in Baltimore. Cempra is currently progressing ophthalmic solithromycin towards an IND.
- In one study, several formulations of 1% solithromycin ophthalmic solution were developed and screened in preclinical models to assess tolerability, and to evaluate achievement of desired PK parameters for an ophthalmic solution. Researchers found solithromycin ophthalmic solution to achieve appropriate concentrations in ocular and periocular tissues, and to be well tolerated with no signs of ocular redness, discomfort or irritation.Clinically relevant concentrations of solithromycin were measured in multiple areas of the eye after a single topical dose while systemic plasma concentrations remained very low, regardless of the evaluated formulation.
- In the other study, researchers assessed the effect of solithromycin on meibomian gland epithelial cells. Meibomian glands, which are found in the eyelids, secrete the lipid layer that protects the ocular tear film from becoming dry. Meibomian gland dysfunction is an important cause of dry eye disease.
- Researchers found that solithromycin induced a rapid and dose dependent increase in healthy secretions from human meibomian gland epithelial cells, in vitro. This response was seen more rapidly than a similar effect observed with azithromycin in the same cell culture system.
Is
general: Yes
