Doxapram

Summary

Doxapram (CHEMBL1754) is an approved small-molecule central nervous system stimulant (ATC R07AB01); indicated across 2 conditions including respiratory system disorder and panic disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R07AB01
• Indications: 2 conditions
• Clinical trials: 8
• Chemistry: 378.5 Da · C24H30N2O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1754
Name	Doxapram
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3156
ChEBI	CHEBI:681848
ATC	R07AB01
Molecular formula	C24H30N2O2
Molecular weight	378.5
InChIKey	XFDJYSQDBULQSI-UHFFFAOYSA-N

SMILES: CCN1CC(C(C1=O)(C2=CC=CC=C2)C3=CC=CC=C3)CCN4CCOCC4

IUPAC name: 1-ethyl-4-(2-morpholin-4-ylethyl)-3,3-diphenylpyrrolidin-2-one

ChEBI definition: A member of the class of pyrrolidin-2-ones that is N-ethylpyrrolidin-2-one in which both of the hydrogens at the 3 position (adjacent to the carbonyl group) are substituted by phenyl groups, and one of the hydrogens at the 4 position is substituted by a 2-(morpholin-4-yl)ethyl group. A central and respiratory stimulant with a brief duration of action, it is used (generally as the hydrochloride or the hydrochloride hydrate) as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering.

Pharmacological roles (ChEBI): central nervous system stimulant.

Also known as: Docatone, Doxapram, doxapram, SID50112713, DOXAPRAM, Doxapram hydrochloride

Parent form; salt/anhydrous children: CHEMBL1200876, CHEMBL3989519

Patent coverage: 525 distinct patent families (2,073 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: 5 (assay-derived). Sample: 5-hydroxytryptamine receptor 2C, Voltage-gated inwardly rectifying potassium channel KCNH2, Cytochrome P450 2D6, Potassium channel subfamily K member 3, Potassium channel subfamily K member 9.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR2C	7.15	AC50	71	nM	CHEMBL_ACT_25131823
CYP2D6	7	IC50	100	nM	CHEMBL_ACT_7679362
O54912	6.39	IC50	410	nM	CHEMBL_ACT_18916528

Target pathways

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

Indications & clinical

Indications

2 indications (1 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
respiratory system disorder	4	MONDO:0005087	EFO:0000684
panic disorder	2	MONDO:0005383	EFO:0004262

Clinical trials

Total trials: 8.

Phase distribution

Phase	Trials
Not specified	3
PHASE4	2
PHASE3	1
PHASE2	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00389909	PHASE4	COMPLETED	Dosing Chart for Calculating the First Dose of Doxapram in Premature Infants
NCT02171910	PHASE4	COMPLETED	Doxapram as an Additive to Propofol Sedation in Sedation for ERCP
NCT04430790	PHASE3	RECRUITING	Doxapram Therapy in Preterm Infants (DOXA Trial)
NCT01022151	PHASE2	COMPLETED	Aminophylline and Cognitive Function After Sevoflurane Anaesthesia
NCT06585163	PHASE1	NOT_YET_RECRUITING	Study to Investigate the Safety, Tolerability and Pharmacokinetics of QEV-817 Oral Suspension
NCT07022704	Not specified	RECRUITING	Doxapram Administration on Diaphragmatic Excursion in Mechanically Ventilated Patients With Chronic Obstructive Pulmonary Disease Undergoing Spontaneous Breathing Trial
NCT02820025	Not specified	UNKNOWN	The Effect and Mechanism of Respiratory Stimulant Doxapram on Facilitating Emergence
NCT03894189	Not specified	UNKNOWN	The Effect of Doxapram Versus Theophylline on Diaphragmatic Function

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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