Dexmecamylamine

Summary

Dexmecamylamine (CHEMBL2103881) is a phase-3 clinical-stage small molecule; indicated across 6 conditions including major depressive disorder and depressive disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 6 conditions
• Clinical trials: 20
• Chemistry: 167.29 Da · C11H21N

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2103881
Name	Dexmecamylamine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	12358972
Molecular formula	C11H21N
Molecular weight	167.29
InChIKey	IMYZQPCYWPFTAG-NGZCFLSTSA-N

SMILES: C[C@@]1([C@@H]2CC[C@@H](C2)C1(C)C)NC

IUPAC name: (1R,2S,4S)-N,2,3,3-tetramethylbicyclo[2.2.1]heptan-2-amine

Also known as: Dexmecamilamina, Dexmecamylamine, NIH-11008, Tc-5214, TC-5214, DEXMECAMYLAMINE

Parent form; salt/anhydrous children: CHEMBL2105753

Patent coverage: 14 distinct patent families (18 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Acetylcholine receptor; alpha1/beta1/delta/gamma, Neuronal acetylcholine receptor; alpha4/beta2, Neuronal acetylcholine receptor; alpha3/beta4, Neuronal acetylcholine receptor subunit alpha-7.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CHRNB4	6.7	IC50	200	nM	CHEMBL_ACT_15023480
CHRNB2	6.3	IC50	500	nM	CHEMBL_ACT_15023482
CHRNA1	6.22	IC50	600	nM	CHEMBL_ACT_15023476
CHRNA7	5.92	IC50	1200	nM	CHEMBL_ACT_15023478

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

6 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
major depressive disorder	3	MONDO:0002009	MONDO:0002009
depressive disorder	3	MONDO:0002050	MONDO:0002050
overactive bladder	2	MONDO:0006624	EFO:1000781
hypertensive disorder	1	MONDO:0005044	EFO:0000537
drug dependence	1	MONDO:0005303	EFO:0003890
kidney disorder	1	MONDO:0005240	EFO:0003086

Clinical trials

Total trials: 20.

Phase distribution

Phase	Trials
PHASE1	9
PHASE3	5
PHASE2	5
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01152554	PHASE3	COMPLETED	A Study to Assess the Long- Term Safety of TC-5214 as an Adjunct Therapy in Patients With Major Depressive Disorder
NCT01153347	PHASE3	COMPLETED	A Study to Assess the Efficacy and Safety of TC-5214 as an Adjunct Therapy in Patients With Major Depressive Disorder
NCT01157078	PHASE3	COMPLETED	A Study to Assess the Efficacy and Safety of TC-5214 as an Adjunct Therapy in Patients With Major Depressive Disorder (MDD)
NCT01180400	PHASE3	COMPLETED	A Study to Assess the Efficacy and Safety of TC-5214 as an Adjunct Therapy in Patients With Major Depressive Disorder
NCT01197508	PHASE3	COMPLETED	A Study to Assess the Efficacy and Safety of TC-5214 as an Adjunct Therapy in Patients With Major Depressive Disorder.
NCT00692445	PHASE2	COMPLETED	TC-5214 as add-on the Treatment of Major Depressive Disorder
NCT00899977	PHASE1/PHASE2	TERMINATED	TC-5214 as Augmentation Therapy in Patients With Refractory Hypertension
NCT01288079	PHASE2	TERMINATED	A Study to Assess the Safety and Effect of TC-5214 in Patients With Major Depressive Disorder.
NCT01868516	PHASE2	COMPLETED	Study Evaluating the Safety, Tolerability, and Efficacy of Dexmecamylamine (TC-5214) for Treatment of Overactive Bladder
NCT03404570	PHASE2	COMPLETED	Exploratory Study to Assess the Efficacy and Safety of TC-5214 in the Treatment of Subjects With Palmar Hyperhidrosis
NCT04263623	PHASE2	UNKNOWN	Clinical Study to Assess the Efficacy and Safety of AT-5214 in the Treatment of Subjects With Palmar Hyperhidrosis
NCT01145768	PHASE1	COMPLETED	To Investigate the Safety and Tolerability of TC-5214 Following Oral Administration of Multiple Doses for up to 8 Days
NCT01175564	PHASE1	COMPLETED	To Investigate Safety, Tolerability and Pharmacokinetics of TC-5214 in Healthy Male Japanese Subjects
NCT01239771	PHASE1	COMPLETED	A Study to Assess Safety and Tolerability as Well as Absorption and Excretion of TC-5214 in Medically Stable Elderly Subjects
NCT01240967	PHASE1	COMPLETED	To Compare the Pharmacokinetics of a Single Oral Dose of TC-5214 in Subjects With Renal Impairment and With Subjects With Normal Renal Function
NCT01359618	PHASE1	TERMINATED	Determining Highest Dose Administration of TC-5214 and Evaluating Effect on the Electrical Activity in the Heart
NCT01392820	PHASE1	COMPLETED	A Study of Single and Multiple Ascending Doses of TC-5214 in Japanese Healthy Elderly Male and Female Volunteers
NCT01403922	PHASE1	TERMINATED	To Determine Blood Pressure Interaction Between TC-5214 and Anti-Hypertensive Medications (Calcium Channel Blockers, Beta Blockers, and ACE Inhibitors) in Patients With Chronic Hypertension
NCT01458899	PHASE1	COMPLETED	Study in Healthy Subjects to Measure the Effects of Food on the Pharmacokinetics of TC-5214
NCT01500018	PHASE1	WITHDRAWN	Study in Healthy Recreational Polydrug Users to Measure the Abuse Potential of TC-5214

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).