Delving into the Latest Updates on Solithromycin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Solithromycin (JAN/USAN), CEM-101, OP-1068

+ [3]

Target

50S subunit

Action

inhibitors

Mechanism

50S subunit inhibitors(50S ribosomal subunit inhibitors), Protein biosynthesis inhibitors

Therapeutic Areas

Infectious DiseasesRespiratory Diseases

Active Indication

Respiratory Tract Infections

Inactive Indication

airway diseaseCommunity Acquired PneumoniaCommunity-acquired bacterial pneumonia+ [3]

Originator Organization

Cubist Pharmaceuticals LLC

Active Organization

FUJIFILM Pharmaceuticals USA, Inc.

Inactive Organization

Melinta Therapeutics, Inc.Cempra Pharmaceuticals, Inc.

License Organization

Cempra Pharmaceuticals Inc.

Optimer Pharmaceuticals LLCToyama Chemical Co., Ltd.

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC43H65FN6O10

InChIKeyIXXFZUPTQVDPPK-ZAWHAJPISA-N

CAS Registry760981-83-7

Novel antimicrobial agents are continually developed to address the global threat of multidrug-resistant Neisseria gonorrhoeae. Promising candidates include zoliflodacin and, possibly, solithromycin. We evaluated their in-vitro activities against gonococcal isolates collected in Korea. In total, 250 N. gonorrhoeae isolates obtained across Korea between 2016 and 2018 were used to determine the minimum inhibitory concentrations (MICs) of 10 therapeutic agents using the CLSI agar dilution method. Most isolates (94.8%, 237/250) demonstrated non-susceptibility to penicillin G, tetracycline, and ciprofloxacin, and susceptibility to ceftriaxone and spectinomycin was substantially high. The half-maximal IC (MIC50) and 90% IC (MIC90) values for zoliflodacin were 0.03 and 0.06 μg/mL, respectively; 0.06 and 0.12 μg/mL, respectively, for solithromycin; and 0.03 and 0.12 μg/mL, respectively, for ceftriaxone. Notably, no cross-resistance was observed between zoliflodacin and ciprofloxacin, despite both targeting DNA topoisomerase II enzymes. Zoliflodacin and solithromycin demonstrated significant in-vitro activity against multidrug-resistant N. gonorrhoeae isolates, and zoliflodacin has shown non-inferiority to ceftriaxone/azithromycin dual therapy in a clinical phase 3 trial. Collectively, our findings highlight the potential of zoliflodacin as a novel therapeutic agent for gonococcal infections, particularly in the context of rising multidrug resistance, and highlight the need for continued surveillance and development of alternative antimicrobial strategies.

01 Aug 2025·Life Science Alliance

Structural studies on ribosomes of differentially macrolide-resistantStaphylococcus aureusstrains

Article

Author: Thompson, Sophie ; Zimmerman, Ella ; Melenitzky, Tal ; Le Scornet, Alexandre ; Rivalta, André ; Hiregange, Disha-Gajanan ; Fedorenko, Aliza ; Çavdaroglu, Sude ; Yap, Mee-Ngan Frances ; Bashan, Anat ; Breiner Goldstein, Elinor ; Yonath, Ada ; Halfon, Yehuda

Antimicrobial resistance is a major global health challenge, diminishing the efficacy of many antibiotics, including macrolides. InStaphylococcus aureus, an opportunistic pathogen, macrolide resistance is primarily mediated by Erm-family methyltransferases, which mono- or dimethylate A2058 in the 23S ribosomal RNA, reducing drug binding. Although macrolide–ribosome interactions have been characterized in nonpathogenic species, their structural basis in clinically relevant pathogens remains limited. In this study, we investigate the impact ofermB-mediated resistance on drug binding by analyzing ribosomes fromS. aureusstrains with varying levels ofermBexpression and activity. Using cryo-electron microscopy, we determined the high-resolution structures of solithromycin-bound ribosomes, including those with dimethylated A2058. Our structural analysis reveals the specific interactions that enable solithromycin binding despite double methylation and resistance, as corroborated by microbiological and biochemical data, suggesting that further optimization of ketolide–ribosome interactions could enhance macrolide efficacy against resistantS. aureusstrains.

04 Nov 2024·CHEMBIOCHEM

Engineering of a Malonyl‐CoA Ligase for Production of Fluorinated Polyketide Extender Units

Article

Author: Williams, Gavin J. ; Paulsel, Thaddeus Q.

Abstract:

Enzymatic platforms for producing malonyl‐CoA‐based extender units required for polyketide biosynthesis are often based on malonyl‐CoA ligases such as MatB from Rhizobium trifolii and Rhodopseudomonas palustris. However, despite broad interest in the fluorination of polyketides and prior success with engineering MatB homologs, the suitability of MatB for accessing the tertiary substituted fluoromethylmalonyl‐CoA needed to produce flurithromycin and solithromycin has not yet been reported. Herein, we report the structure‐guided engineering of a MatB homolog to optimize the production of fluoromethylmalonyl‐CoA, resulting in a variant with increased conversion and providing a platform to produce a suitable building block mixture for fluorinated macrolide production. Additionally, the mutant demonstrated broad utility for various substituted malonyl‐CoAs. The MatB mutant sets the stage to access fluorinated macrolides by coupling it with altered PKS machinery to install fluorinated malonyl‐CoA into macrolide scaffolds.

7

News (Medical) associated with Solithromycin

20 Nov 2025

·investors.edgewisetx.com

Edgewise Therapeutics Appoints Commercial Biotech Executive Christopher Martin to its Board of Directors

BOULDER, Colo., Nov. 20, 2025 /PRNewswire/ -- Edgewise Therapeutics, Inc., (Nasdaq: EWTX), a leading muscle disease biopharmaceutical company, today announced the appointment of biotechnology veteran Christopher Martin to its Board of Directors. Mr. Martin brings proven success across all key commercial functions, including marketing, sales, commercial operations, market access, trade and business development. "We are thrilled to welcome Chris to our Board of Directors," said Kevin Koch, Ph.D., President and Chief Executive Officer. "His commercial expertise and launch leadership will be critical as we prepare for our first commercial launch in Becker muscular dystrophy and advance our cardiovascular asset to Phase 3. Prior to joining the Edgewise Board, Mr. Martin served as Chief Commercial Officer for Verona Pharma, which was acquired by Merck & Co. for approximately $10 billion in October of 2025. As CCO, Mr. Martin was responsible for building the commercial organization and launch strategy for the company's first product launch, Ohtuvayre® (ensifentrine). Prior, he served as Executive Director of Marketing at SK Life Science which is focused on developing novel therapeutics for central nervous system conditions. Mr. Martin was instrumental in developing the commercial and marketing strategy and the framework for launching their first commercial product, XCOPRI® (cenobamate tablets). Until its acquisition by Melinta Therapeutics, Mr. Martin was Head of Marketing at Cempra where he led the development and launch strategy for the company's first product, solithromycin. Prior to Cempra, he was at Salix Pharmaceuticals for 10 years in roles of increasing responsibility and led the Xifaxan® marketing team during the company's acquisition by Valeant Pharmaceuticals. Mr. Martin received a Bachelor of Science in Financial Management from Clemson University. About Edgewise Therapeutics Edgewise Therapeutics is a leading muscle disease biopharmaceutical company developing novel therapeutics for muscular dystrophies and serious cardiac conditions. The Company's deep expertise in muscle physiology is driving a new generation of novel therapeutics. Sevasemten is an orally administered first-in-class fast skeletal myosin inhibitor in late-stage clinical trials in Becker and Duchenne muscular dystrophies. EDG-7500 is a novel cardiac sarcomere modulator for the treatment of hypertrophic cardiomyopathy and other diseases of diastolic dysfunction, currently in Phase 2 clinical development. EDG-15400 is a novel cardiac sarcomere modulator for the treatment of heart failure, currently in Phase 1 clinical development. The entire team at Edgewise is dedicated to our mission: changing the lives of patients and families affected by serious muscle diseases. To learn more, go to: www.edgewisetx.com or follow us on LinkedIn, X, Facebook and Instagram. Cautionary Note Regarding Forward-Looking Statements This press release contains forward-looking statements as that term is defined in Section 27A of the Securities Act of 1933 and Section 21E of the Securities Exchange Act of 1934. Statements in this press release that are not purely historical are forward-looking statements. Such forward-looking statements include, among other things, statements regarding the potential of, and expectations regarding, Edgewise's product candidates and programs, including sevasemten, EDG-7500 and EDG-15400; statements regarding Edgewise's ability to commercialize sevasemten; statements regarding Edgewise's ability to advance its cardiovascular asset to Phase 3; and statements by Edgewise's President and Chief Executive Officer. Words such as "believes," "anticipates," "plans," "expects," "intends," "will," "goal," "potential" and similar expressions are intended to identify forward-looking statements. The forward-looking statements contained herein are based upon Edgewise's current expectations and involve assumptions that may never materialize or may prove to be incorrect. Actual results could differ materially from those projected in any forward-looking statements due to numerous risks and uncertainties, including but not limited to: risks associated with Edgewise's limited operating history, its products being early in development and not having products approved for commercial sale; risks associated with Edgewise not having generated any revenue to date; Edgewise's ability to achieve objectives relating to the discovery, development and commercialization of its product candidates, if approved; Edgewise's need for substantial additional capital to finance its operations; Edgewise's substantial dependence on the success of sevasemten and EDG-7500; Edgewise's ability to develop and commercialize sevasemten, EDG-7500 and EDG-15400; risks related to Edgewise's clinical trials of its product candidates not demonstrating safety and efficacy; risks related to Edgewise's product candidates causing serious adverse events, toxicities or other undesirable side effects; the outcome of preclinical testing and early clinical trials not being predictive of the success of later clinical trials and the risks related to the results of Edgewise's clinical trials not satisfying the requirements of regulatory authorities; delays or difficulties in the enrollment and/or maintenance of patients in clinical trials; risks related to failure to capitalize on other indications or product candidates; risks related to competition; risks relating to interim, topline and preliminary data from Edgewise's clinical trials changing as more patient data becomes available; risks related to failure to develop a proprietary drug discovery platform; risks related to exposure to additional risk if we develop sevasemten and potential other programs in connection with other therapies; risks related to production of drugs by Edgewise's third-party manufacturers; risks related to changes in methods of product candidate manufacturing or formulation; risks related to not achieving adequate market acceptance; risks related to the patient population for our product candidates having a small patient population; risks related to the regulatory approval processes of domestic and foreign authorities being lengthy, time consuming and inherently unpredictable; risks relating to disruptions at the FDA, the SEC and other government agencies; risks relating to Edgewise's ability to attract and retain highly skilled executive officers and employees; Edgewise's ability to obtain and maintain intellectual property protection for its product candidates; Edgewise's reliance on third parties; risks related to future acquisitions or strategic partnerships; risks related to general economic and market conditions; and other risks. Information regarding the foregoing and additional risks may be found in the section entitled "Risk Factors" in documents that Edgewise files from time to time with the U.S. Securities and Exchange Commission. These forward-looking statements are made as of the date of this press release, and Edgewise assumes no obligation to update the forward-looking statements, or to update the reasons why actual results could differ from those projected in the forward-looking statements, except as required by law. View original content to download multimedia:https://www.prnewswire.com/news-releases/edgewise-therapeutics-appoints-commercial-biotech-executive-christopher-martin-to-its-board-of-directors-302620999.html SOURCE Edgewise Therapeutics

Phase 1Phase 2Executive ChangeAcquisition

30 Mar 2023

·www.drugs.com

Not Enough Antibiotics in Drug Development Pipeline, WHO Says

THURSDAY, March 30, 2023 -- Only 12 new antibiotics entered the market between 2017 and 2021, and too few currently are under development against critical pathogens, according to a World Health Organization presentation at the 33rd European Congress of Clinical Microbiology & Infectious Diseases, held from April 15 to 18 in Copenhagen, Denmark. Valeria Gigante, Ph.D., from the WHO Antimicrobial Resistance Division in Geneva, and colleagues updated the state of the antibiotic landscape. They reported that of the 12 antibiotics approved, only cefiderocol is able to target all the pathogens deemed critical by WHO. Of the 27 antibiotics currently under development, only solithromycin, which is used to treat community-acquired pneumonia and other infections, is awaiting market authorization and seven are in phase 3 trials. Only four of the 27 have new mechanisms of action, and most are not new drug classes. Only six of the 27 are considered innovative enough to overcome antibiotic resistance using WHO criteria, and only two of the six target highly drug-resistant forms of these microbes. "There is a major gap regarding products addressing multidrug resistant pathogens, such as Acinetobacter baumannii and Pseudomonas aeruginosa ," Gigante said in a statement. "Few new innovative antibiotics are expected in the coming years. We have no silver bullets." More Information Posted March 2023

Phase 3Qualified Infectious Disease Product

29 Dec 2016

·www.biospace.com

FDA Rejects Cempra’s NDAs for Solithromycin, Shares Sink

December 29, 2016 By Mark Terry , BioSpace.com Breaking News Staff Cempra , headquartered in Chapel Hill, NC, announced today that it had received a Complete Response Letter (CRL) from the U.S. Food and Drug Administration (FDA) concerning its new drug applications (NDAs) for its antibiotic solithromycin. Solithromycin, both oral and intravenous, was being evaluated for the treatment of community-acquired bacterial pneumonia (CABP) in adults. The FDA indicated it could not approve the NDAs in their current form. The agency also requested more clinical safety data and a resolution to inspection deficiencies found at the company’s manufacturing facility. It did not request more efficacy data. Of particular concern was insufficient characterization of hepatotoxicity. The company stated, “The FDA noted the size of the safety database is limited to 920 patients who received solithromycin at the proposed dose and duration, and is too small to adequately characterize the nature and frequency of serious hepatic adverse effects.” The FDA recommended a comparative study, as well as a study of about 9,000 patients, to exclude serious drug induced liver injury (DILI) at a rate of about 1:3000 with a 95 percent probability. The manufacturing concerns arose during inspections of the Wockhardt Limited and Pfizer ’s Hospira, Inc. manufacturing plants. The company plans to meet with the FDA as soon as possible to discuss the issues, as well as the design of future clinical safety studies. Cempra also will give the FDA an update on manufacturing progress at Uquifia, an alternate GMP manufacturing plant for solithromycin active pharmaceutical ingredient (API). Uquifia is in India-based Vivimed Labs Ltd ’s Spanish business. “As the rates of antibiotic resistance continue to rise, there is an unmet medical need for new antibiotics to treat patients with CABP and Cempra is committed to working with the FDA to achieve the approval of solithromycin as quickly as possible,” said David Zaccardelli , acting chief executive officer of Cempra, in a statement. Cempra plunged at the news, dropping approximately 130 percent to a current value of $2.65. Zaccardelli also stated, “With more than $225 million of cash on hand, patent protection for solithromycin through 2032 and a pipeline that includes fusidic acid and other potential programs for solithromycin, including an ophthalmic formulation, we have flexibility to determine the best course forward for solithromycin and Cempra.” Fusidic acid is Cempra’s second lead product candidate. It has completed enrollment of a Phase III clinical trial in patients with acute bacterial skin infections. It is also evaluating a study of the drug for refractory infections in bones and joints. There is some speculation that Cempra will abandon solithromycin development. At a conference call, Zaccardelli indicated that they wouldn’t know what the cost of a new trial would be until after meetings with the FDA. Andrew Berens , an analyst with Morgan Stanley , predicted in a note to clients that due to the size and cost of the study, as well as the probability of restrictive labeling were the drug to be approved, that the company will likely halt development of solithromycin.

Phase 3

100 Deals associated with Solithromycin

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External Link

KEGG	Wiki	ATC	Drug Bank
D09965	Solithromycin	J01FA16	DB09308

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Community Acquired Pneumonia	NDA/BLA	United States	Melinta Therapeutics, Inc.	20 Jan 2016
Respiratory Tract Infections	Phase 3	Japan	FUJIFILM Pharmaceuticals USA, Inc.	30 Jan 2022
Gonococcal urethritis	Phase 3	United States	Melinta Therapeutics, Inc.	01 Aug 2014
Gonococcal urethritis	Phase 3	Australia	Melinta Therapeutics, Inc.	01 Aug 2014
Community-acquired bacterial pneumonia	Phase 3	United States	Melinta Therapeutics, Inc.	01 Dec 2012
Community-acquired bacterial pneumonia	Phase 3	Argentina	Melinta Therapeutics, Inc.	01 Dec 2012
Community-acquired bacterial pneumonia	Phase 3	Bulgaria	Melinta Therapeutics, Inc.	01 Dec 2012
Community-acquired bacterial pneumonia	Phase 3	Canada	Melinta Therapeutics, Inc.	01 Dec 2012
Community-acquired bacterial pneumonia	Phase 3	Czechia	Melinta Therapeutics, Inc.	01 Dec 2012
Community-acquired bacterial pneumonia	Phase 3	Dominican Republic	Melinta Therapeutics, Inc.	01 Dec 2012

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02628769 (CTgov)	Phase 2	Pulmonary Disease, Chronic Obstructive \| airway disease	6	Solithromycin (Solithromycin)	llyqlhaelo(cbdmssgknj) = txcxlijgfw kzbxujgnvn (tmxerhjgaa, 0.76) View more	-	30 Dec 2019
				Placebo (Placebo)	llyqlhaelo(cbdmssgknj) = ekqqxkewzm kzbxujgnvn (tmxerhjgaa, 1.21) View more
NCT02210325 (Pubmed \| Lancet Infect Dis) Manual	Phase 3	Gonorrhea First line	261	solithromycin	zpztusmutr(krjxpkizgn) = ykyfgunrjp iawvmvwciu (chvpgmlbpf ) View more	Negative	01 Aug 2019
				ceftriaxone+azithromycin	zpztusmutr(krjxpkizgn) = exhwkydmgp iawvmvwciu (chvpgmlbpf ) View more
NCT02605122 (CTgov)	Phase 2/3	Community-acquired bacterial pneumonia	97	Solithromycin (Solithromycin)	askbttejgh = htylktjiam nxepuspmeg (opsgsotbmm, qrsohdomlc - jzwuvsjkux) View more	-	03 Jan 2019
				Standard of Care (Standard of Care)	askbttejgh = yckdthuklk nxepuspmeg (opsgsotbmm, xtigscgule - wrzibulzsu) View more
NCT01968733 (SOLITAIRE-IV, Pubmed \| Clin Infect Dis) Manual	Phase 3	Community-acquired bacterial pneumonia	863	Solithromycin	uhvoopthnk(jpboxoslwg) = qlzplertce ywsphrrtqi (yacapjvaix ) View more	Non-inferior	15 Oct 2016
				Moxifloxacin	uhvoopthnk(jpboxoslwg) = ffxelmmwil ywsphrrtqi (yacapjvaix ) View more
NCT01756339 (SOLITAIRE-ORAL, Pubmed \| Lancet Infect Dis) Manual	Phase 3	Community-acquired bacterial pneumonia	860	Placebo+solithromycin	ocjajgtixq(kbrolsjzvj) = dvaytmphkt lskewzbpjr (sgpwprhnik ) View more	Non-inferior	01 Apr 2016
				moxifloxacin	ocjajgtixq(kbrolsjzvj) = igjzcxbfag lskewzbpjr (sgpwprhnik ) View more
NCT01966055 (Pubmed \| Antimicrob Agents Chemother)	Phase 1	-	13	Solithromycin	ncvwagcrwg(jgrsuxfygr) = quarsqurod ubgihgbplt (ypqbbmzksp, 0.61)	-	01 Apr 2016
NCT01591447 (Pubmed \| Clin Infect Dis)	Phase 2	Gonorrhea	59	Solithromycin 1200 mg	yyydzrnrox(jzkusbkuuc) = jwbywnlbpb ldpyrzxpua (kiyvnxwcco ) View more	Positive	01 Oct 2015
ERS2015	Phase 3	Pulmonary Disease, Chronic Obstructive \| Asthma \| Community Acquired Pneumonia	860	Oral solithromycin	fiklmjqceo(ybyktjizsd) = 36.6% vs 35.6% of patients experienced adverse events with Oral solithromycin vs Oral moxifloxacin lgdmjgugqz (uymiagshln ) View more	-	01 Sep 2015
				Oral moxifloxacin
NCT01168713 (Pubmed \| Antimicrob Agents Chemother)	Phase 2	Community-acquired bacterial pneumonia	132	Solithromycin 800 mg	qbpaldexuz(myfaymuilg) = rcewzqyxmd snsriekzuu (rjizczzhsk ) View more	-	01 Jun 2013
				Levofloxacin 750 mg	qbpaldexuz(myfaymuilg) = mfmuxjhifu snsriekzuu (rjizczzhsk ) View more