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Expert Opin Ther Pat. 2011 Jan;21(1):85-101. doi: 10.1517/13543776.2011.536532. Epub 2010 Nov 19.

T-type calcium channels inhibitors: a patent review.

Author information

1
AstraZeneca R&D, Lead Generation, SE-431 83 Mölndal, Sweden. fabrizio.giordanetto@astrazeneca.com

Abstract

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.

PMID:
21087200
DOI:
10.1517/13543776.2011.536532
[Indexed for MEDLINE]

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