Drugs / Loperamide
Loperamide
also known as
imodium · Loperamide hydrochloride · Arret · Chlorhydrate of Loperamide · Diah-limit · Diaquitte · Diareze · Diarrhoea relief · +28 more
Small molecule targets OPRM1 via activation
Regulatory milestones approvals, filings & regulatory actions · 2 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Label expansion | US (FDA) | IMODIUM A-D | — | 1992-11-23 | fda.gov ↗ |
| Approved | US (FDA) | IMODIUM | — | 1976-12-28 | fda.gov ↗ |
Trials 31
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 01 trial · 1 met primary | ||||||
| Phase 0 | NCT02711891 | Mar → Dec 2015 | — | Rush University Medical Center | Completed | Met primary |
| Phase 17 trials | ||||||
| Phase 1 | NCT05252546 | Mar → Aug 2022 | HER2 positive breast carcinoma | Jiangsu HengRui Medicine Co., Ltd. | Completed | No outcome recorded |
| Phase 1 | NCT04315116 | Apr 2020 | — | Jiangsu HengRui Medicine Co., Ltd. | Completed | No outcome recorded |
| Phase 1 | NCT04225078 | Jan 2020 → Dec 2021 | — | Janssen Research & Development, LLC | Completed | No outcome recorded |
| Phase 1 | NCT04186936 | Dec 2019 | — | McNeil AB | Completed | No outcome recorded |
| Phase 1 | NCT02677844 | Feb → Jul 2016 | — | Eli Lilly and Company | Completed | No outcome recorded |
| Phase 1 | NCT00806299 | Nov 2008 | — | Johnson & Johnson Consumer and Personal Products Worldwide | Completed | No outcome recorded |
| Phase 1 | NCT02251119 | Jul 2002 → Jan 2003 | — | Boehringer Ingelheim | Completed | No outcome recorded |
| Phase 1/21 trial | ||||||
| Phase 1/2 | NCT04823065 | Sep 2018 → Aug 2023 | endometrial cancer, ovarian cancer | Centre de recherche du Centre hospitalier universitaire de Sherbrooke | Completed | No outcome recorded |
| Phase 25 trials | ||||||
| Phase 2 | NCT07426822 | Apr 2026 → Apr 2027 expected | hormone receptor-positive breast cancer | Maryam Lustberg | Not yet recruiting | No outcome recorded |
| Phase 2 | NCT05252988 | Aug 2022 → Oct 2024 overdue | HER2 positive breast carcinoma, female breast carcinoma, hormone receptor-positive breast cancer | Spanish Breast Cancer Research Group | Active not recruiting | No outcome recorded |
| Phase 2 | NCT05154396 | Jan 2022 → Dec 2023 | HER2 positive breast carcinoma | Chinese Academy of Medical Sciences | Unknown | No outcome recorded |
| Phase 2 | NCT04576208 | Nov 2020 → Jul 2022 | non-small cell lung carcinoma | Takeda | Withdrawn | No outcome recorded Stop: Business |
| Phase 2 | NCT02400476 | Feb 2015 → Apr 2021 | HER2 positive breast carcinoma | Puma Biotechnology, Inc. | Completed | No outcome recorded |
| Phase 2/32 trials · 1 missed | ||||||
| Phase 2/3 | NCT04736186 | May 2020 → Oct 2022 | breast cancer | Tianjin Medical University Cancer Institute and Hospital | Unknown | No outcome recorded |
| Phase 2/3 | NCT02099006 | Nov 2013 → Jun 2015 | female reproductive system disorder | University of Rochester | Completed | Missed primary |
| Phase 35 trials · 1 missed | ||||||
| Phase 3 | NCT02263365 | Oct 2014 → Dec 2016 | diversion colitis | Cedars-Sinai Medical Center | Terminated | No outcome recorded |
| Phase 3 | NCT02008565 | Feb 2014 → May 2016 | — | NICHD Pelvic Floor Disorders Network | Completed | Missed primary |
| Phase 3 | NCT01814553 | Apr 2013 → Jul 2015 | non-small cell lung carcinoma | Boehringer Ingelheim | Completed | No outcome recorded |
| Phase 3 | NCT00444093 | Mar 2007 → Feb 2008 | cancer, diarrheal disease, enteritis | Philipps University Marburg | Terminated | No outcome recorded Stop: Enrollment |
| Phase 3 | NCT00003057 | Mar 1997 → May 2000 | colorectal cancer, diarrheal disease | Eastern Cooperative Oncology Group | Completed | No outcome recorded |
| Phase 45 trials · 1 met primary | ||||||
| Phase 4 | NCT00933465 | Oct 2009 → May 2010 | — | University Hospital Southampton NHS Foundation Trust | Withdrawn | No outcome recorded |
| Phase 4 | NCT00807326 | Nov 2008 → Aug 2009 | diarrheal disease | McNeil AB | Completed | Met primary |
| Phase 4 | NCT00685607 | Oct 2008 | acute diarrhea | Johnson & Johnson Consumer and Personal Products Worldwide | Completed | No outcome recorded |
| Phase 4 | NCT00292344 | Jun 2004 → Aug 2005 | acute diarrhea | The University of Texas Health Science Center, Houston | Completed | No outcome recorded |
| Phase 4 | NCT00359970 | Jun 2002 → Aug 2003 | diarrheal disease | The University of Texas Health Science Center, Houston | Completed | No outcome recorded |
| Phase not applicable5 trials · 1 missed | ||||||
| — | NCT03501498 | Apr 2017 → May 2018 | — | University Hospital Plymouth NHS Trust | Completed | No outcome recorded |
| — | NCT01780909 | Feb → Dec 2013 | — | KU Leuven | Unknown | No outcome recorded |
| — | NCT01717456 | Jan 2013 → Mar 2015 | — | University of North Carolina, Chapel Hill | Terminated | Missed primary Stop: Enrollment |
| — | NCT01618591 | Sep 2012 → Mar 2016 | dysentery | Uniformed Services University of the Health Sciences | Terminated | No outcome recorded Stop: Enrollment |
| — | NCT02165475 | May 2002 → Mar 2005 | — | University Hospital, Linkoeping | Completed | No outcome recorded |
| Comparator or background therapy35 trials | ||||||
| Phase 1 | NCT05528848 Background | Sep 2022 → Sep 2027 expected | substance-related disorder | University of Pennsylvania | Active not recruiting | No outcome recorded |
| Phase 1 | NCT04038619 Background | Feb 2021 → Dec 2027 expected | breast cancer, cervical cancer, colitis, diarrheal disease +4 | M.D. Anderson Cancer Center | Recruiting | No outcome recorded |
| Phase 1 | NCT02057133 Background | Mar 2014 → Mar 2021 overdue | breast neoplasm | Eli Lilly and Company | Active not recruiting | No outcome recorded |
| Phase 1 | NCT01596764 Comparator | May → Jul 2011 | intestinal obstruction | University Medicine Greifswald | Completed | No outcome recorded |
| Phase 1 | NCT01596777 Comparator | Jan → Mar 2010 | intestinal obstruction | University Medicine Greifswald | Completed | No outcome recorded |
| Phase 1 | NCT00954304 Background | Jun → Aug 2009 | — | Hanmi Pharmaceutical Company Limited | Completed | No outcome recorded |
| Phase 1/2 | NCT02858310 Background | Jan 2017 → Jul 2025 | cervical intraepithelial neoplasia, human papilloma virus infection, in situ carcinoma, vulvar neoplasm | National Cancer Institute (NCI) | Completed | No outcome recorded |
| Phase 2 | NCT06865677 Background | Jun → Jul 2025 | cervical carcinoma, endometrial carcinoma, ovarian carcinoma | National Cancer Institute (NCI) | Terminated | No outcome recorded |
| Phase 2 | NCT05520723 Background | Feb → Oct 2023 | hormone receptor-positive breast cancer, triple-negative breast carcinoma | MedSIR | Completed | No outcome recorded |
| Phase 2 | NCT04366713 Background | Jun 2020 → Dec 2021 | HER2 positive breast carcinoma | Puma Biotechnology, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT04172597 Background | Dec 2019 → Mar 2022 | breast cancer, colorectal cancer, glioblastoma | Spectrum Pharmaceuticals, Inc | Terminated | No outcome recorded Stop: Business |
| Phase 2 | NCT03094052 Background | Oct 2018 → Oct 2022 | HER2 positive breast carcinoma, breast adenocarcinoma | University of California, San Francisco | Completed | No outcome recorded |
| Phase 2 | NCT03705442 Background | Feb 2018 → Feb 2020 | colorectal cancer | Marin Golčić | Unknown | No outcome recorded |
| Phase 2 | NCT02747004 Background | Sep 2016 → Jun 2018 overdue | breast cancer | Eli Lilly and Company | Active not recruiting | Missed primary |
| Phase 2 | NCT02441946 Background | Aug 2015 → Aug 2016 | hormone receptor-positive breast cancer | Eli Lilly and Company | Completed | Met primary |
| Phase 2 | NCT02323516 Comparator | Dec 2014 → Dec 2015 | cancer | Centre Francois Baclesse | Withdrawn | No outcome recorded |
| Phase 2/3 | NCT02686645 Background | Dec 2016 → Dec 2021 | Clostridium difficile colitis | Queen Elizabeth II Health Sciences Centre | Unknown | No outcome recorded |
| Phase 2/3 | NCT01350570 Comparator | Aug 2011 → Feb 2014 | functional diarrhea, irritable bowel syndrome | Chengdu University of Traditional Chinese Medicine | Completed | No outcome recorded |
| Phase 2/3 | NCT00727649 Comparator | Jul 2008 → Oct 2013 | — | US Department of Veterans Affairs | Completed | No outcome recorded |
| Phase 3 | NCT02354768 Background | Oct 2015 → Dec 2017 | — | University Hospital, Strasbourg, France | Terminated | No outcome recorded |
| Phase 3 | NCT02266849 Comparator | Oct 2014 → Aug 2015 | rectal cancer, short bowel syndrome, ulcerative colitis | Odense University Hospital | Terminated | No outcome recorded Stop: Enrollment |
| Phase 3 | NCT02340481 Comparator | Jul 2005 → May 2006 | diarrheal disease | Xian-Janssen Pharmaceutical Ltd. | Completed | No outcome recorded |
| Phase 3 | NCT00650637 Background | Jan → Aug 2003 | diarrheal disease | Pfizer | Terminated | No outcome recorded |
| Phase 4 | NCT06148025 Background | Nov 2023 → Oct 2027 expected | — | South Australian Health and Medical Research Institute | Recruiting | No outcome recorded |
| Phase 4 | NCT05677282 Background | Oct 2022 → Sep 2025 overdue | acute diarrhea | Henry M. Jackson Foundation for the Advancement of Military Medicine | Recruiting | No outcome recorded |
| Phase 4 | NCT02217982 Comparator | Jul 2014 → Jun 2015 | relapsing-remitting multiple sclerosis | Rocky Mountain MS Research Group, LLC | Terminated | No outcome recorded Stop: Enrollment |
| Phase 4 | NCT03017430 Background | Jan 2014 → Dec 2019 | substance withdrawal syndrome | St. Petersburg Bekhterev Research Psychoneurological Institute | Completed | No outcome recorded |
| Phase 4 | NCT00591357 Comparator | Oct 2007 → Dec 2013 | Clostridium difficile colitis, diarrheal disease | Michael E. DeBakey VA Medical Center | Suspended | No outcome recorded |
| — | NCT06424522 Background | Feb 2027 → Dec 2028 expected | rectal carcinoma | Ohio State University Comprehensive Cancer Center | Recruiting | No outcome recorded |
| — | NCT07635394 Background | Apr 2026 overdue | irritable bowel syndrome | Beijing Tiantan Hospital | Recruiting | No outcome recorded |
| — | NCT06892093 Background | Aug 2025 → Jun 2027 expected | HER2 positive breast carcinoma, diarrheal disease | Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Recruiting | No outcome recorded |
| — | NCT06235931 Background | Feb 2024 → Dec 2025 overdue | breast neoplasm | Second Affiliated Hospital of Soochow University | Recruiting | No outcome recorded |
| — | NCT05920681 Background | Jun 2023 → May 2025 | — | National Cancer Center Affiliate of Vilnius University Hospital Santaros Klinikos | Unknown | No outcome recorded |
| — | NCT03215017 Comparator | May 2017 → Dec 2022 | — | Mirna Abraham-Nordling | Completed | No outcome recorded |
| — | NCT02888899 Background | Mar 2016 → Mar 2018 | — | University Hospital, Linkoeping | Unknown | No outcome recorded |
News releases announcing trial results or a regulatory action · 6
| Date | Issuer | Release |
|---|---|---|
| 2023-03-28 | Zydus Lifesciences Limited | Regulatory Zydus receives Final Approval from the USFDA for Loperamide Hydrochloride Capsules USP, 2 mg zyduslife.com ↗
Zydus Lifesciences Limited (including its subsidiaries/affiliates, hereinafter referred to as “Zydus”) has received final approval for Loperamide Hydrochloride Capsules USP, 2 mg (USRLD: Imodium® Capsules) from the United States Food and Drug Administration (USFDA). |
| 2020-08-19 | Puma Biotechnology, Inc. | Results Puma Biotechnology Announces Publication of Interim Results of Phase II CONTROL Trial in Annals of Oncology - CONTROL Trial Investigates Anti-diarrheal Strategies Including Dose Escalation in Neratinib-treated Patients with Early Stage HER2-positive Breast Cancer - Dose Escalation Resulted in Reduced Rate, Severity and Duration of Grade ≥3 Diarrhea Compared to Phase III ExteNET Trial, Lower Diarrhea-related Discontinuations and Dose Reductions in Multiple CONTROL Cohorts pumabiotechnology.com ↗
The most significant impact was seen using a dose escalation strategy with loperamide as needed, which included utilizing a lower dose of neratinib during the first two weeks of a 52-week treatment period. |
| 2019-10-02 | Puma Biotechnology, Inc. | Results FDA Approves Labeling Supplement for Puma Biotechnology’s NERLYNX® (neratinib) for the Extended Adjuvant Treatment of HER2-Positive Early Stage Breast Cancer Interim data from the Phase II CONTROL Trial showed that the addition of prophylactic treatment with loperamide plus budesonide reduced the rate of discontinuation due to neratinib-associated diarrhea to 11% versus a discontinuation rate of 18% with loperamide alone. pumabiotechnology.com ↗
Interim data from the trial showed that the addition of prophylactic treatment with loperamide plus budesonide reduced the discontinuation rate due to neratinib-associated diarrhea to 11% versus a discontinuation rate of 18% with loperamide alone. |
| 2018-09-07 | Perrigo Company | Regulatory Perrigo Announces Final FDA Approval and Planned Launch for the Store Brand OTC Equivalent of Imodium® Multi-Symptom Relief perrigo.com ↗
Perrigo Company plc (NYSE; TASE: PRGO) today announced that it has received final approval from the U.S. Food & Drug administration for the store brand over-the-counter (OTC) equivalent of Imodium ® Multi-Symptom Relief (loperamide hydrochloride and simethicone tablets, 2 mg/125 mg). |
| 2017-04-04 | Puma Biotechnology, Inc. | Results Puma Biotechnology Presents Interim Results of Phase II CONTROL Trial of PB272 in Extended Adjuvant Treatment of HER2-Positive Early Stage Breast Cancer at the 2017 AACR Annual Meeting pumabiotechnology.com ↗
The presentation entitled, “Effects of adding budesonide or colestipol to loperamide prophylaxis on neratinib-associated diarrhea in patients with HER2-positive early stage breast cancer: the CONTROL trial,” was presented as a poster presentation. |
| 2016-12-08 | Puma Biotechnology, Inc. | Results Puma Biotechnology Presents Interim Results of Phase II CONTROL Trial of PB272 in Extended Adjuvant Treatment of HER2-Positive Early Stage Breast Cancer at the 2016 San Antonio Breast Cancer Symposium pumabiotechnology.com ↗
The interim analysis of the trial presented in the poster included a total of 135 patients who received neratinib plus loperamide prophylaxis (28 patients taking the original dosing and 107 patients taking the modified dosing) and 40 patients who received neratinib plus loperamide prophylaxis for 2 cycles and budesonide for 1 cycle. |
All press releases naming this drug 7 releases
Evidence & citations 41 cited values
Every value below carries the sentence it was read from. 67 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | Loperamide | “Loperamide prophylaxis: 4mg three times daily on days 1-14 and 4mg twice daily on days 15-56, followed by as needed, not exceeding 16mg/ day.” NCT05154396 ↗59“Loperamide: 2-4 mg after each loose stool (max 16 mg/day) to reduce stool frequency, though it does not relieve pain” NCT07635394 ↗ “Medication to help control of the bowel movement (One or a combination of Loperamide, Sorbitol, Sterculia gum)” NCT03215017 ↗ “Antidiarrheal prophylaxis includes loperamide tablet administered as per routine clinical practice.” NCT04576208 ↗ “Drug: Loperamide” NCT07426822 ↗ |
| Known as | Arret | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Chlorhydrate of Loperamide | “* Chlorhydrate of Loperamide (2 mg capsule or tablet) 6 / day for 72 hours (D0 to D3)” NCT02354768 ↗ |
| Known as | Diah-limit | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Diaquitte | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Diareze | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Diarrhoea relief | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Diasorb | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Diocalm | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Diocaps | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Dioraleze | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Entrocalm | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Gppe pack | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | imodium | “Antidiarrheal regimen 1: Oral imodium (2 tablets/times, 2 times a day) from the first week, 1 tablet, 2 times a day from the second week.” NCT06235931 ↗4“Loperamide is a standard treatment for diarrhea, and is available over the counter under the name, Imodium.” NCT00591357 ↗ “rapidly acting loperamide (imodium) combined with curative dose of the poorly absorbed rifaximin” NCT00292344 ↗ “Imodium at a starting dose of 2 mg/day may be used for diarrhea if unresponsive to fiber.” NCT01717456 ↗ “Imodium (Loperamide Hydrochloride) syrup” NCT00933465 ↗ |
| Known as | Imodium (loperamide) | “Imodium (loperamide)” NCT01717456 ↗ |
| Known as | Imodium a-d | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Imodium a-d ez chews | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Imodium advanced | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Imodium classic | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Imodium ibs relief | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Imodium instant melts | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Imodium instants | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Imodium liquicaps | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Lodiar | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Loperagen | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Loperamid | ClinicalTrials.gov intervention name — accepted as the source's own label NCT00444093 ↗ |
| Known as | Loperamida | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Loperamide hcl | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Loperamide hydrochloride | “Imodium (Loperamide Hydrochloride) syrup” NCT00933465 ↗ |
| Known as | Loperamide hydrochloride component of imodium multi-symptom relief | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Loperamidi hydrochloridum | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Loperamidum | “Loperamidum Dosage form: Loperamide Tablets (2mg of loperamide hydrochloride.). Dosage: Initial dose - 2 tablets immediately, then - 1 tablet after each loose stool, but not...” NCT05920681 ↗ |
| Known as | Norimode | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Normaloe | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | NSC-696356 | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | R 18,553 | ChEMBL registry synonym — accepted as the source's own label CHEMBL841 ↗ |
| Known as | Seldiar | “loperamide ("Seldiar")” NCT03705442 ↗ |
| Action | Activate | “Loperamide is an opioid agonist” NCT01596777 ↗1“Mu opioid receptor agonist” CHEMBL841 ↗ |
| Modality | Small molecule | “Loperamide, a piperdine derivative with a structure similar to the synthetic opioid meperidine” NCT02711891 ↗ |
| Route | Oral | “Patients in arm C receive oral doses of loperamide following each unformed stool for 5 days” NCT00003057 ↗ |
| Target | OPRM1 | “Mu opioid receptor agonist” CHEMBL841 ↗ |