pentoxiverine

Small moleculeexperimental

Pentoxyverine is a non-opioid antitussive used to prevent cough caused by common cold. It is used as an active ingredient of several oral over-the-counter cough suppressants alone or in combination with other medications, especially decongestants. Certuss is a combination of pentoxyverine and guaifenesin. Pentoxyverine is FDA pregnancy category C drug. Known as anticonvulsant, and spasmolytic agent. — NCATS

Clinical trial activity

1 trials · 1 clinical orgs · 0 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Nov 1, 2009 (NCT02183649)

Timeline

2000s

Jan 1, 2009
Earliest Phase 1 Sponsor(trial)

Indications

Approved for

Sinusitis

Studied for

Mechanism of action

Sigma opioid receptorAGONIST
SIGMAR1 agonist
Carbetapentane suppresses the cough reflex in the central nervous system, but the exact mechanism of action is not known with certainty. The drug acts as an agonist at sigma receptors (subtype ¿1).
Binding affinity (determined by competitive binding to [3H]-pentazocine-labelled sites on guinea-pig brain membranes): 75+- 28 nM, n=3
- Sigma non-opioid intracellular receptor 1 (SIGMAR1) ↗

Chemistry & pharmacology

Loading structure…

SMILES

CCN(CC)CCOCCOC(=O)C1(c2ccccc2)CCCC1

Mol. weight: 333.47 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No
Delivery: Oral

Oral

Yes

Parenteral

Topical

Sources

Also known as

1-phenylcyclopentanecarboxylic acid,2-(2-(diethylamino)ethoxy)ethyl ester
2-(2-diethylaminoethoxy)ethyl 1-phenylcyclopentyl-1-carboxylate
carbetapentane
carbetapentane
carbetapentane
carbetapentane
carbetapentane
carbetapentane
carbetapentane
carbetapentane 1,5-napthalenedisulfonate (2:1)
carbetapentane 2,6-napthalenedisulfonate (2:1)
carbetapentane citrate
carbetapentane citrate
carbetapentane citrate
carbetapentane citrate
carbetapentane tannate
pentoxiverine
pentoxyverine
pentoxyverine
pentoxyverine
pentoxyverine
pentoxyverine
pentoxyverine
pentoxyverine citrate
pentoxyverine citrate
pentoxyverine citrate
pentoxyverine citrate
toclase
toclase

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT02183649	Phase 1	Nov 1, 2009	Boehringer Ingelheim

Showing 1 of 1 trials

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Organizations

Research & Development (1)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Boehringer Ingelheim	For profit	1	1	1	2009

1 organizations

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