Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance

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...

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Autores principales:	Muhammad Habiburrahman, Vivian Soetikno, Wani Riselia Sirait, Missy Savira
Formato:	article
Lenguaje:	EN
Publicado:	Universitas Gadjah Mada 2020
Materias:	antibiotic cem-101 gonorrhea solithromycin resistance Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/cbae30110717402d9df5f0d7e0a579cb
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spelling	oai:doaj.org-article:cbae30110717402d9df5f0d7e0a579cb2021-11-15T06:08:47ZSolithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance2338-94272338-948610.22146/ijp.1123https://doaj.org/article/cbae30110717402d9df5f0d7e0a579cb2020-12-01T00:00:00Zhttps://jurnal.ugm.ac.id/v3/IJP/article/view/1123https://doaj.org/toc/2338-9427https://doaj.org/toc/2338-9486Gonorrhea 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%).Muhammad HabiburrahmanVivian SoetiknoWani Riselia SiraitMissy SaviraUniversitas Gadjah Madaarticleantibioticcem-101gonorrheasolithromycinresistancePharmacy and materia medicaRS1-441ENIndonesian Journal of Pharmacy, Pp 335–353-335–353 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	antibiotic cem-101 gonorrhea solithromycin resistance Pharmacy and materia medica RS1-441
spellingShingle	antibiotic cem-101 gonorrhea solithromycin resistance Pharmacy and materia medica RS1-441 Muhammad Habiburrahman Vivian Soetikno Wani Riselia Sirait Missy Savira Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
description	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%).
format	article
author	Muhammad Habiburrahman Vivian Soetikno Wani Riselia Sirait Missy Savira
author_facet	Muhammad Habiburrahman Vivian Soetikno Wani Riselia Sirait Missy Savira
author_sort	Muhammad Habiburrahman
title	Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_short	Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_full	Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_fullStr	Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_full_unstemmed	Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_sort	solithromycin as a potential novel antibiotic against neisseria gonorrhoeae resistance
publisher	Universitas Gadjah Mada
publishDate	2020
url	https://doaj.org/article/cbae30110717402d9df5f0d7e0a579cb
work_keys_str_mv	AT muhammadhabiburrahman solithromycinasapotentialnovelantibioticagainstneisseriagonorrhoeaeresistance AT viviansoetikno solithromycinasapotentialnovelantibioticagainstneisseriagonorrhoeaeresistance AT waniriseliasirait solithromycinasapotentialnovelantibioticagainstneisseriagonorrhoeaeresistance AT missysavira solithromycinasapotentialnovelantibioticagainstneisseriagonorrhoeaeresistance
_version_	1718428581414043648

Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance

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