Proprietary Discovery Platform

  PRODUCT/INDICATION PRE CLINICAL PHASE 1 PHASE 2 PHASE 3 NDA Submitted FDA Approved
Radezolid: 2nd generation oxazolidinone for acne vulgaris
Topical
ESKAPE* Program: novel pyrrolocytosine
“SUPER-BUGS”
Macrolide Program
NEXT-GEN
PRODUCT/INDICATION DELIVERY/PHASE
Proprietary Discovery Platform
Radezolid: 2nd generation oxazolidinone
TOPICAL, ACNE / Phase 1
ESKAPE* Program: novel pyrrolocytosine
“SUPER-BUGS” / Preclinical
Macrolide Program
NEXT-GEN / Preclinical
  • ESKAPE: The ESKAPE pathogen is methicillin-resistant Staphylococcus aureus
  • QIDP: Qualified Infectious Disease Product || SPA: Special Protocol Assessment

Multiple Candidates in Pre-clinical and Clinical Studies

Melinta Therapeutics’ early stage pipeline also includes novel compounds in established antibiotic classes in preclinical and clinical testing. The Oxazolidinone Program and Macrolide Program utilize the Company’s proprietary technology that allows for the precise targeting of binding sites within the bacterial ribosomes to improve and optimize drug properties and performance.

Radezolid: a Second-Generation Oxazolidinone

Radezolid is a second-generation oxazolidinone; Melinta scientists analyzed the ribosomal binding region of oxazolidinones with an aim to create compounds with higher binding affinity to overcome resistance to linezolid, minimal off-target activity, a pharmacokinetic profile supporting intravenous or oral bioavailability and a broader spectrum of antimicrobial activity than is currently available in the class.

An oral formulation of radezolid was assessed in two Phase 2 clinical trials in uncomplicated skin and skin structure infections and in community acquired bacterial pneumonia. In these studies, radezolid showed encouraging clinical cure rates and activity against a number of pathogens. Additionally, radezolid was well tolerated, with the most commonly reported adverse events being gastrointestinal symptoms.

In January 2015, Melinta entered into a license agreement for the development and commercialization of radezolid in topical formulations for a variety of dermatological indications. Melinta retains the option to co-develop or fully regain rights to radezolid upon completion of specific development milestones. This innovative deal structure creates multiple potential options for realizing long-term financial return for Melinta. Melinta recently announced the successful completion of a Phase 1 study to investigate radezolid for the treatment of acne vulgaris and the initiation of a Phase 2 proof of concept study.

ESKAPE Program

eskape pathogen program videoIn addition to our late stage portfolio, we have an active research platform based on Nobel Prize-winning science and a powerful, proprietary drug discovery platform. In our ESKAPE Pathogen Program, we are focused on developing breakthrough antibiotics for bacterial “superbugs”. ESKAPE pathogens include Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter species and Escherichia coli.

Our goal is to introduce completely novel classes of antibiotics to meet the challenge posed by the alarming emergence of bacteria that have developed resistance to all existing drug classes. Currently these pathogens cause mortality rates approaching 50 percent in some infection types, making “superbugs” the most serious hospital-treated bacterial threat. In addition, the causative pathogen is often unknown, creating the need for therapies that cover the full range of potential bacteria.

We have successfully designed three novel classes of antibiotics that show potent activity in the laboratory and in animal infection models. In our lead class, known as the pyrrolocytosines, several compounds have demonstrated comprehensive activity across the full set of bacterial “superbugs.” We believe this new class of antibiotic could be transformational in the fight against this urgent threat. Based on significant recent progress, our ESKAPE Pathogen Program is poised to deliver compounds to enter development in 2016 for advancement to human clinical trials in 2017.

Click here to visit the ESKAPE Pathogen Program Publications webpage.

As with other existing classes of antibiotics, bacterial resistance is growing to the widely used macrolide class. In our Macrolide program, we have created enhanced macrolides that overcome resistance, have a broader spectrum of antimicrobial activity than current macrolides, and retain or improve the properties for an oral therapy. Currently, compounds in the Macrolide Program have the potential to treat the bacteria typically identified in skin and lung infections in the community and hospital as well as respiratory disease in the animal health arena.

Macrolide Program

As with other existing classes of antibiotics, bacterial resistance is growing to the widely used macrolide class. In our Macrolide program, we have created enhanced macrolides that overcome resistance, have a broader spectrum of antimicrobial activity than current macrolides, and retain or improve the properties for an oral therapy. Currently, compounds in the Macrolide Program have the potential to treat the bacteria typically identified in skin and lung infections in the community and hospital as well as respiratory disease in the animal health arena.