Diphenoxylate

Summary

Diphenoxylate (CHEMBL1201294) is an approved small-molecule antidiarrhoeal drug (ATC A07DA01).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A07DA01
• Clinical trials: 5
• Chemistry: 452.6 Da · C30H32N2O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201294
Name	Diphenoxylate
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	13505
ChEBI	CHEBI:4639
ATC	A07DA01
Molecular formula	C30H32N2O2
Molecular weight	452.6
InChIKey	HYPPXZBJBPSRLK-UHFFFAOYSA-N

SMILES: CCOC(=O)C1(CCN(CC1)CCC(C#N)(C2=CC=CC=C2)C3=CC=CC=C3)C4=CC=CC=C4

IUPAC name: ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-carboxylate

ChEBI definition: A piperidinecarboxylate ester that is the ethyl ester of difenoxin.

Pharmacological roles (ChEBI): antidiarrhoeal drug.

Also known as: Difenoxilato, Diphenoxylate, IDS-ND-016, SID50113007, DIPHENOXYLATE, LOMOTIL

Parent form; salt/anhydrous children: CHEMBL1200665

Patent coverage: 4,419 distinct patent families (15,776 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: 2 (assay-derived). Sample: Mu-type opioid receptor, Potassium voltage-gated channel subfamily A member 3.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
OPRM1	7.91	Ki	12.37	nM	CHEMBL_ACT_24411911
KCNA3	5.3	IC50	5000	nM	CHEMBL_ACT_12188984

Target pathways

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

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 5.

Phase distribution

Phase	Trials
PHASE2	3
PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00583323	PHASE3	COMPLETED	Diphenoxylate / Atropine to Decrease FDG Activity During F-18 FDG PET
NCT01391962	PHASE2	COMPLETED	Sunitinib or Cediranib for Alveolar Soft Part Sarcoma
NCT01851369	PHASE1/PHASE2	COMPLETED	TRC102 and Temozolomide for Relapsed Solid Tumors and Lymphomas
NCT03094052	PHASE2	COMPLETED	Incidence and Severity of Diarrhea in Patients With HER2 Positive Breast Cancer Treated With Trastuzumab and Neratinib
NCT06865677	PHASE2	TERMINATED	Sacituzumab Govitecan for Relapsed Ovarian, Endometrial, and Cervical Carcinomas

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).