Drug name
Cabotegravir Stearate (M2CAB)
Developer(s)
Drug information
Not provided
Cabotegravir Stearate
Not provided
Small molecule
Cabotegravir Stearate (M2CAB) is a novel prodrug of the HIV-1 integrase strand transfer inhibitor (INSTI) cabotegravir (CAB). CAB is indicated as single agent pre-exposure prophylaxis (PrEP) for HIV prevention and is utilised in combination with Rilpivirine (a non-nucleoside reverse transcriptase inhibitor, NNRTI) for HIV treatment. M2CAB is formulated as a nanocrystalline intramuscular long-acting injectable suspension (XVIR-110) that could potentially be dosed once or twice yearly in humans based on pharmacokinetic modelling. M2CAB forms macrophage-distributed and local depots with an apparent protracted elimination half-life resulting in "flip-flop" plasma pharmacokinetics. In preclinical studies, XVIR-110 showed sustained CAB exposures and a favourable injection site reaction profile.
Cabotegravir Stearate (M2CAB) is currently in preclinical development and is not yet approved.
Unknown
Therapeutic area(s)
- HIV
- Pre-Exposure Prophylaxis (PrEP)
- Treatment
Administration route
Intramuscular
Associated long-acting platforms
Aqueous drug particle suspension, Nanocrystal Suspension
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
Not provided
Dosage
Not yet available
Preliminary preclinical data indicates once or twice yearly administration.
Not yet available
M2CAB is formulated as a nanocrystalline intramuscular long-acting injectable suspension (XVIR-110) that has the potential to be dosed once or twice yearly in humans based on pharmacokinetic modelling
The estimated elimination half-life of CAB from XVIR-110 is ~120 days (~17 weeks or ~4 months) and provided mean CAB concentrations greater than 10x & 4x the PB-IC90 for more than 6 months & 1 year.
Formulations
Compare
Cabotegravir Stearate (M2CAB)
Cabotegravir Ultra Long-Acting (CAB-ULA)
Cabotegravir and Rilpivirine
Associated technologies
Not provided
Comment & Information
Developer(s)
Exavir Therapeutics is a biopharmaceutical company focused on developing ultra-long-acting therapeutics for chronic viral infections and CNS disorders. Headquartered in San Francisco, CA, they utilize prodrug nano-formulation technology to extend the half-life of drugs. Their current research focus primarily targets HIV, with the goal of improving treatment adherence and patient outcomes.
Drug structure
Scale-up and manufacturing prospects
Cabotegravir stearate (M2CAB) is currently in preclinical development, therefore detailed manufacturing and scale-up prospects are not currently available. One formulation (XVIR-110) is a nanocrystalline cabotegravir prodrug that achieves and maintains sustained cabotegravir exposures which support its ongoing development as a potential ultra-long-acting INSTI for HIV PrEP and in-combination for treatment.
Not provided
Not provided
Not provided
Excipients
Not provided
Not provided
Not provided
Delivery device(s)
No delivery device
There are either no relevant patents or these were not yet submitted to LAPaL
Publications
There are no publication
Additional documents
No documents were uploaded
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