Drug name
Last update: Jul 2026Sorfequiline (TBAJ-876) tartrate
Developer(s)
Drug information
Not provided
Sorfequiline tartrate; TBAJ-876 LAI
Sorfequiline
Small molecule
Diarylquinoline antimycobacterial agent
High-concentration aqueous LAI suspensions of TBAJ-876 tartrate were developed using wet media milling. Drug concentrations up to 650 mg/mL (free-base equivalent) were achieved while maintaining injectability and acceptable physical properties. The formulation comprised TBAJ-876 tartrate particles stabilized with polysorbate 20 in citrate buffer. Peak plasma concentrations (Cmax) ranged from ~165–268 ng/mL, depending on particle size, with AUC0–3 months of 42,500–49,100 ng·h/mL. Plasma concentrations were sustained for at least 3 months after a single injection.
Not yet approved. Although the non-LAI formulation of TBAJ-876 is currently being evaluated in ongoing clinical trials (NCT06058299 and NCT07672405), the LAI formulation remains under preclinical investigation.
Not approved yet
Therapeutic area(s)
- TB
- Treatment
Administration route
Intramuscular
Associated long-acting platforms
Aqueous drug particle suspension
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
- To be determined
- Other/Variable/Unknown : Unknown
- Every 3 months
Dosage
Dose: 28 mg; Strengths: 280 mg/mL (Preclinical dosage)
652 mg/mL (highest injectable concentration tested)
0.1 ml of Sorfequiline 280 mg/mL (free-base equivalent) was administered via intramuscular (IM) injection to rats. Drug concentrations were monitored for up to three months.
Not provided
Not provided
Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
TB Alliance
TB Alliance, formally known as the Global Alliance for TB Drug Development, is a not-for-profit product development partnership dedicated to the discovery, development, and delivery of faster-acting, safer, and affordable treatments for tuberculosis (TB). Since its establishment in 2000, the organization has played a pivotal role in advancing TB drug research and has built the largest pipeline.
Drug structure
Scale-up and manufacturing prospects
Not provided
1. Standard reaction vessels/flasks 2. Rotary evaporator 3. Filtration setup 4. Drying chamber 5. Dual centrifuge wet media mill 6. Yttrium-stabilized zirconia milling beads
Manufacturing is required to be conducted in Grade C/D cleanroom environments 1. Vehicle preparation 2. Wet media milling (critical step) 3. Particle-size characterization 4. Bulk suspension holding 5. Sterile manufacture / aseptic processing 6. Fill-finish 7. Final product is lyophilized and reconstitution is required before use
1. Mastersizer 3000 laser diffraction analyzer 2. X-ray Powder Diffraction (XRPD) 3. Scanning Electron Microscopy (SEM) 4. High-Performance Liquid Chromatography (HPLC) 5. Osmometer
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
Not provided
Not provided
Not provided
There are either no relevant patents or these were not yet submitted to LAPaL