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T-type calcium channels inhibitors: a patent review
Fabrizio Giordanetto1, Laurent Knerr, Andreas Wållberg
1AstraZeneca R&D, Lead Generation, SE-431 83 Mölndal, Sweden. fabrizio.giordanetto@astrazeneca.com
Importance Of The Field:
T-type calcium channels are transmembrane proteins that regulate calcium entry in the cell in a voltage-dependent manner. Intracellular calcium levels are the key to many physiological processes, ranging from neuron firing to cardiac pacemaking. Inhibition of T-type calcium channels is heralded as a potential treatment to peripheral and CNS disorders, including hypertension, heart failure, sleep, epilepsy, drug addiction and neuropathic pain.
Areas Covered In This Review:
A comprehensive summary of patent literature disclosing T-type calcium channels inhibitors is provided.
What The Reader Will Gain:
In all, 46 patent applications including 15 chemical structure classes are reviewed. Available in vitro, in vivo and clinical results are also discussed.
Take Home Message:
Several selective T-type calcium channels inhibitors with demonstrated in vitro and in vivo effects, including one Phase I clinical candidate, are now available. While future clinical results will be paramount to assess target validity in patients, these novel inhibitors represent excellent tools to further investigate the role of T-type channels in pathophysiological conditions.
Insights
Novel T-type calcium channel inhibitors show promise for treating various disorders. Patent reviews reveal selective inhibitors with demonstrated effects, including a Phase I clinical candidate, offering new research tools.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Neuroscience
Background:
- T-type calcium channels regulate cellular calcium influx, crucial for physiological functions like neuronal firing and cardiac rhythm.
- Inhibiting T-type calcium channels is a promising therapeutic strategy for neurological and cardiovascular conditions.
Purpose of the Study:
- To comprehensively review patent literature on T-type calcium channel inhibitors.
- To assess the potential of these inhibitors in treating various diseases.
Main Methods:
- Systematic review of patent applications related to T-type calcium channel inhibitors.
- Analysis of 15 distinct chemical structure classes of inhibitors.
- Evaluation of available in vitro, in vivo, and clinical data.
Main Results:
- 46 patent applications detailing T-type calcium channel inhibitors were reviewed.
- Selective inhibitors with proven in vitro and in vivo efficacy were identified.
- One inhibitor has advanced to Phase I clinical trials.
Conclusions:
- Selective T-type calcium channel inhibitors are emerging as viable therapeutic agents.
- These novel compounds serve as valuable tools for exploring T-type channel roles in disease.
- Further clinical data is essential to confirm therapeutic efficacy in patients.
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