Solithromycin as a potential novel antibiotic against Neisseria gonorrhoeae resistance
File(s)
Published version
Author(s)
Habiburrahman, Muhammad
Soetikno, Vivian
Sirait, Wani Riselia
Savira, Missy
Type
Journal Article
Abstract
Gonorrhea is one of the most often sexually transmitted infection in the world. In 2016, WHO stated the Southeast Asia region as the fourth-highest incidence rate and prevalence of gonorrhea. One of the current problems with gonorrhea is related to its emerging resistance to first-line drugs such as cephalosporins, macrolides, and fluoroquinolones. This resistance has an impact on the difficulty of finding effective antibiotics to eradicate the infection, thus risking financial loss and infertility in sexually active age patients. This literature review will discuss solithromycin, the first fluoroketolide in phase III clinical trial, and show its potential as a new antibiotic against infection with resistant Neisseria gonorrhoeae. Literatures are searched using Pubmed and Google Scholar search engines with keywords: antibiotics, CEM-101, clinical trial, Neisseria gonorrhoeae, new treatment, pharmacology, pharmacokinetics, resistance, safety, and solithromycin. This semisynthetic antibiotic is supported by a different chemical structure from previous macrolides; improving solithromycin becomes more stable and able to bind easier with bacterial ribosomes. Pharmacologically, solithromycin provides an advantage in its high bioavailability, easy oral administration route, wide distribution, metabolism mainly in the liver, but not required dosage adjustments due to hepatic impairment, and a single dosage preparation that can increase patient compliance in healing gonorrhea infections. Also, its lower MIC50 than previous antibiotics makes it well-tolerated, therefore making this antibiotic as a potential recommendation for the management of multi-drug resistant gonorrhea in the future. Solithromycin is not inferior to the standard therapy (ceftriaxone and azithromycin), with 80% vs. 84% gonorrhea eradication rates. Per the anatomic site, the eradication rate is 92% in genital, 94% in the pharynx, and 83% in the rectum. However, special attention needs to be paid to the side effects of the gastrointestinal tract of solithromycin, as observed in phase III clinical trials at a dose of 1000 mg in the form of diarrhea (24%) and nausea (21%).
Date Issued
2020-12-29
Date Acceptance
2020-12-30
Citation
Indonesian Journal of Pharmacy, 2020, 31 (4), pp.335-353
ISSN
2338-9427
Publisher
Universitas Gadjah Mada
Start Page
335
End Page
353
Journal / Book Title
Indonesian Journal of Pharmacy
Volume
31
Issue
4
Copyright Statement
Copyright (c) 2020 Indonesian Journal of Pharmacy
Creative Commons License
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License.
Creative Commons License
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License.
License URL
Identifier
http://dx.doi.org/10.22146/ijp.1123
Publication Status
Published
Date Publish Online
2020-12-28