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Safety and Pharmacokinetics Study of Naldemedine in Paediatric Participants Receiving Opioids

Phase 1
Recruiting
Conditions
Opioid-Induced Constipation (OIC)
Interventions
Registration Number
NCT05588323
Lead Sponsor
Shionogi
Brief Summary

The primary objective of this study is to evaluate the pharmacokinetic (PK) profile of naldemedine and nor-naldemedine after a single oral dose of naldemedine in pediatric participants who are receiving or about to receive opioids.

Detailed Description

Not available

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
24
Inclusion Criteria

Disease Characteristics

  • Participants with cancer or non-cancer pain who are receiving (or who are about to receive) acute or chronic treatment with opioids.
  • Participants with either newly diagnosed constipation, a history of constipation treated with laxatives, or are expected to develop constipation after opioid treatment.
  • Able to remain in the clinic for blood sampling for at least 12 hours following the first study intervention dose and are able to return for blood sampling at the 24-hour time point.

Weight

  • Body mass index within approximately the 3rd to 97th percentile for their age according to the World Health Organization Child Growth Standards.
Exclusion Criteria

Medical Conditions

  • History of a gastrointestinal (GI) neoplasm or an ongoing GI-related issue or any recent (within last 1 year) or planned GI tract surgery.
  • Signs or symptoms of GI obstruction or participants with recurrent obstruction who may be at increased risk of GI perforation.
  • Inability to eat/swallow or have need of a nasogastric tube.
  • No bowel movements reported for 7 consecutive days at the time of obtaining informed consent or on the initial day of study intervention administration (Study Day 1).
  • History of more than 1 week of Common Terminology Criteria for Adverse Events (CTCAE) Grade 3 neutropenia or thrombocytopenia with clinical sequelae.
  • Participants who need mechanical ventilation.
  • Severe CTCAE Grade 3 or above hepatic or renal impairment including end-stage renal disease requiring hemodialysis, as determined by the investigator.
  • Progressive neurological disorders or potential disruption to the blood-brain barrier (for example, primary brain malignancies, central nervous system metastases, active multiple sclerosis, etc.) considering the risk of opioid withdrawal or reduced analgesia.

Prior/Ongoing Medications

  • Currently receiving the first cycle of chemotherapy.
  • Previously received naldemedine.

Other Exclusions

  • Positive pregnancy test for females of childbearing potential.

Note: Other protocol-defined Inclusion/Exclusion criteria may apply.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Cohort 1: ≥ 12 to < 18 YearsNaldemedineParticipants will receive 0.05 milligrams (mg) to 0.2 mg naldemedine based on their body weight once daily for 7 days.
Cohort 2: ≥ 6 to < 12 YearsNaldemedineParticipants will receive 0.05 mg to 0.2 mg naldemedine based on their body weight once daily for 7 days.
Cohort 3: ≥ 2 to < 6 YearsNaldemedineParticipants will be enrolled in this cohort after the safety and PK data has been evaluated for cohorts 1 and 2. Participants will receive 0.05 mg to 0.2 mg naldemedine based on their body weight once daily for 7 days.
Primary Outcome Measures
NameTimeMethod
Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration (AUC0-last) of Naldemedine and Nor-naldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Metabolic Ratio of Cmax of Nor-naldemedine to Cmax of Naldemedine (MRM/U, Cmax) for Nor-naldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Maximum Plasma Concentration (Cmax) of Naldemedine and Nor-naldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Time to Achieve Maximum Plasma Concentration (Tmax) of Naldemedine and Nor-naldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
AUC Extrapolated From Time Zero to Infinity (AUC0-inf) of Naldemedine and Nor-naldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Apparent Total Clearance (CL/F) of NaldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Mean Residence Time (MRT) of NaldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Metabolic Ratio of AUC of Nor-naldemedine to AUC of Naldemedine (MRM/U, AUC) for Nor-naldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Apparent Volume of Distribution in the Terminal Phase (Vz/F) of NaldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Terminal Elimination Rate Constant (λz) of Naldemedine and Nor-naldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Terminal Elimination Half-life (t1/2,z) of Naldemedine and Nor-naldemedineDay 1: 0.5, 1, 5, and 12 hours postdose; Day 2: 24 hours post Day 1 dose, before administering the Day 2 dose; Day 7 (Cohort 1 only): Predose and 1 hour postdose
Secondary Outcome Measures
NameTimeMethod
Number of Participants Experiencing Treatment-emergent Adverse EventsDay 1 through Day 7
Population PK Analysis: Tmax of NaldemedineDay 1 through Day 7
Population PK Analysis: Cmax of NaldemedineDay 1 through Day 7
Population PK Analysis: Accumulation Ratio for Cmax Calculated as Ratio of Day 7 to Day 1 Cmax (RCmax) of NaldemedineDay 1 through Day 7
Population PK Analysis: AUC From Time Zero to tau (AUC0-tau) of NaldemedineDay 1 through Day 7
Population PK Analysis: Accumulation Ratio for AUC Calculated as Ratio of Day 7 to Day 1 AUC (RAUC) of NaldemedineDay 1 through Day 7
Palatability of Naldemedine Powder for Oral Suspension in Participants Aged 6 Years and AboveDay 1 through Day 7

Palatability will be assessed by participant self-reporting using a visual analogue scale (VAS).

Palatability of Naldemedine Powder for Oral Suspension in Participants Aged 2 to Less Than 6 YearsDay 1 through Day 7

Palatability will be assessed by the investigator or a participant's parent/legal guardian and, if possible, by participant self-reporting using a VAS with facial hedonic scale.

Ability to Swallow Naldemedine TabletsDay 1 through Day 7

Ability to swallow will be assessed by self-reported ease of swallowing after the first dose. Willingness to swallow will be assessed based on the participant's behavior indicative of a negative response and the response to the taste of naldemedine powder for oral suspension formulation compared to the participant's response to all other oral medications currently being given.

Trial Locations

Locations (16)

University Center Mother Theresa , Hospital - Onco-hematology department

🇦🇱

Tirana, Albania

Yeolyan Hematology. , and Oncology Center -

🇦🇲

Yerevan, Armenia

CHU Saint-Pierre Clinical Trials Unit

🇧🇪

Brussels, Belgium

Universitair Ziekenhuis Brussel (UZBrussel) - Department of Anesthesiology and Perioperative Medicine

🇧🇪

Brussels, Belgium

University Hospitals Leuven Pediatrisch hemato-oncology

🇧🇪

Leuven, Belgium

University Clinical Hospital , Mostar

🇧🇦

Mostar, Bosnia and Herzegovina

Hôpital Béclère Service de Pédiatrie Centre de Référence des Maladies Héréditaires du Métabolisme Hépatique (CRMHMH)

🇫🇷

Clamart, France

Hôpital Jeanne de Flandre Antenne du CIC pédiatrique - Niveau 0 CHU de Lille

🇫🇷

Lille, France

Hôpital Armand Trousseau Service Hématologie et Oncologie Pédiatrique

🇫🇷

Paris, France

Instituto Nazionale dei Tumori

🇮🇹

Milan, Italy

Citta della Salute e della Scienza di Torino

🇮🇹

Torino, Italy

Maternal and Child Health Institute IRCCS Burlo Garofolo, Pain and pediatric palliative care service

🇮🇹

Trieste, Italy

National Center for Child Health and Development

🇯🇵

Tokyo, Japan

PHI University Clinic for Children's , Surgery

🇲🇰

Skopje, North Macedonia

University Clinic for Childrens Diseases , Department of Oncology, Hematology and , Malignant Hemopathy

🇲🇰

Skopje, North Macedonia

Chu de Caen

🇫🇷

Caen, France

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