Diphenoxylate · Diphenoxylate Hydrochloride And Atropine Sulfate, Isopto Atropine

What is Diphenoxylate?

Diphenoxylate is a piperidine derivative chemically related to meperidine that acts on opioid receptors in the gastrointestinal tract to decrease motility and prevent diarrhea.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as

Diphenoxylate Hydrochloride And Atropine Sulfate, Isopto Atropine, Lomotil

Drug type

Small molecule

Targets

opioid receptors

Mechanism

Agonist of opioid receptors

Pathways

gastrointestinal motility

Therapy area

Oncology

Developer

Pfizer

In trials of

PBYI

FDA status

Approved as Diphenoxylate Hydrochloride And Atropine Sulfate, Isopto Atropine, Lomotil (September 15, 1960), NDA012462 · FDA label

UNII

73312P173G

✅ FDA-approved uses

• Diarrhea (Diphenoxylate Hydrochloride And Atropine Sulfate)
• Diarrhea (Lomotil)

From the indications section of the FDA label (version of Feb 23, 2026). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Breast AdenocarcinomaHER2-positive Breast CancerStage II Breast Cancer AJCC v6 and v7Stage IIA Breast Cancer AJCC v6 and v7Stage IIB Breast Cancer AJCC v6 and v7Stage III Breast Cancer AJCC v7Stage IIIA Breast Cancer AJCC v7Stage IIIB Breast Cancer AJCC v7Stage IIIC Breast Cancer AJCC v7

Sources

• FDA label (DailyMed)
• FDA label Diphenoxylate Hydrochloride And Atropine Sulfate (2026-02-23), indications
• FDA label Lomotil (2026-02-23), indications
• FDA label Isopto Atropine (2022-10-07), indications
• NCI Thesaurus
• ClinicalTrials.gov NCT03094052

Updated Oct 3, 2026.