Drug name
Last update: Aug 2026ELQ-331
Drug information
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ELQ-331
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Small molecule
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ELQ-331, also known as MMV167, is an alkoxycarbonate ester prodrug of the P. falciparum cytochrome bc1 inhibitor ELQ-300 (MMV055) currently in preclinical development for malaria chemoprevention. ELQ-330 displays potent activity versus blood & liver stages of P. falciparum, however, prodrug approaches are required to mitigate its adverse physiochemical properties including poor water solubility & high crystallinity. ELQ-331 displays improved oral bioavailability and a reduced capacity to develop insoluble crystals compared with ELQ-300. Despite this, ELQ-331 is relatively hydrophobic in nature which introduces challenges regarding oral dosing. Therefore, it is postulated that ELQ-331 exhibits favourable pharmacokinetic and pharmacodynamic properties for long-acting injectable delivery.
Unknown
Unknown
Therapeutic area(s)
- Malaria
- Pre-Exposure Prophylaxis (PrEP)
Administration route
Intramuscular, Oral
Associated long-acting platforms
Polymer-based particles, Aqueous drug particle suspension
Use of drug
- Administered by a nurse
- Administered by a specialty health worker
- Self-administered
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Dosage
Not provided
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Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
Oregon Health Sciences University
Oregon Health & Science University (OHSU) is Oregon's premier public research institution dedicated to health sciences. Established in 1887, OHSU boasts a renowned research environment tackling critical health challenges across neuroscience, cancer biology & infectious diseases. Nationally recognized for its research output, its collaborative environment fosters innovation in the healthcare space.
Medicines for Malaria Venture
MMV is a Swiss-based not-for-profit organization working through a product development partnership model to deliver a portfolio of accessible medicines with the power to treat, prevent and eliminate malaria. We close critical gaps in research, development and access – working “end-to-end” to expand the use of existing antimalarials and innovate new compounds to protect public health.
Drug structure
Scale-up and manufacturing prospects
ELQ-331 can be formulated utilising spray-dried dispersion (SDD) or self-emulsifying drug delivery system (SEDDS) approaches to improve solubility and bioavailability. Spray-drying technology is amenable to production scale-up and is suitable for continuous processing, which could potentially facilitate the industrial manufacture of ELQ-331. The SEDDS formulation method displayed a narrow particle distribution, small emulsion droplet sizes & good self-emulsifying properties. Testing of SEDDS formulations in rat models showed a 1.4-fold increase in ELQ-300 levels compared with the SDD approach.
For SDD Formulations: (1) Industrial-scale spray-dryer, (2) Scintillation vials, (3) Laboratory mixer, (4) Laboratory desiccator and (5) Soluplus® (Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer). For SEDDS Formulations: (1) Titration apparatus, (2) Vortex mixer and (3) Aeroperl® 300 Pharma (Colloidal silicon dioxide).
Spray-dried formulations of ELQ-331 were created through dissolution of the drug and polymer (Soluplus®) in organic solvent. Following this, insoluble granulated high purity colloidal silicon dioxide (Aeroperl® 300 Pharma) was dispersed and spray dried into a powder. The SDD powder is shelf stable and showed no signs of degradation after ambient storage for twelve weeks under closed and open cap conditions. SEDDS formulations were achieved by assessing ELQ-331 solubility in surfactants, co-surfactants and oils. From here, a suitable combination of premix was identified for SEDDS generation.
For SDD Formulation: (1) HPLC to assess drug content. (2) Fourier transform infrared spectroscopy to detect chemical changes. (3) Differential scanning calorimetry and Powder X-ray diffraction (PXRD) to identify presence/absence of crystallinity. (4) Thermogravimetric analysis for thermal stability studies. For SEDDS Formulation: (1) Dynamic light scattering nanoparticle size analyzer (e.g. Horiba LB-550, Sunnyvale, CA) to determine droplet size and distribution. (2) HPLC to characterise the overall formulation.
Excipients & delivery device(s)
No proprietary excipient used
No novel excipient or existing excipient used
No residual solvent used
No delivery device
Safety, Efficacy and Evidence Summary
Not provided
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ELQ-331 compound as broad Markush structure
Disclosed are derivative compounds of ELQ-300 that include an ester at position 4. These compounds have enhanced properties relative to ELQ-300. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treating and preventing malaria infections involving administering the pharmaceutical compositions to the subject.
WO2017015360
Compound
Univ Oregon Health & Science; US Gov Veterans Affairs
Not provided
July 27, 2036
Only granted in the US (US10584098B2)