MedPath

Efficacy, Safety, and Pharmacokinetics of Sugammadex (MK-8616) for Reversal of Neuromuscular Blockade in Pediatric Participants Aged Birth to <2 Years (MK-8616-169)

Registration Number
NCT03909165
Lead Sponsor
Merck Sharp & Dohme LLC
Brief Summary

This study will evaluate the efficacy, safety, and pharmacokinetics (PK) of sugammadex (MK-8616) for reversal of both moderate and deep neuromuscular blockade (NMB) in pediatric participants aged birth to \<2 years. The primary hypothesis of this study is that sugammadex is superior to neostigmine in reversing moderate NMB as measured by time to neuromuscular recovery.

Detailed Description

This trial will be conducted in two parts: Part A and Part B. In Part A, PK sampling will be conducted to identify the pediatric dose providing sugammadex exposure comparable to the next oldest age cohort. For Part B participants, the efficacy of sugammadex (i.e. neuromuscular recovery / time to extubation) will be assessed. Further, safety analyses will be conducted in both Parts A and B. Following completion of Part A, an interim analysis (IA) of the PK and safety data will be performed. Once the appropriate doses are confirmed and safety data is assessed for the 2 doses of sugammadex, then Part B will commence.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
137
Inclusion Criteria
  • Categorized as American Society of Anesthesiologists (ASA) Physical Status Class 1, 2, or 3.
  • Has a planned non-emergent surgical procedure or clinical situation (e.g., intubation) that requires moderate or deep NMB with either rocuronium or vecuronium.
  • Has a surgical procedure or clinical situation that would allow neuromuscular monitoring techniques to be applied for neuromuscular transmission monitoring.
  • Is male or female, between birth and <2 years of age.
Exclusion Criteria
  • Is a preterm infant or neonate <36 weeks gestational age at birth.
  • Has any clinically significant condition or situation (e.g., anatomical malformation that complicates intubation) other than the condition requiring the use of NMBA that, in the opinion of the investigator, would interfere with the trial evaluations or optimal participation in the trial.
  • Has a neuromuscular disorder that may affect NMB and/or trial assessments.
  • Is dialysis-dependent or has (or is suspected of having) severe renal insufficiency.
  • Has or is suspected of having a family or personal history of malignant hyperthermia.
  • Has or is suspected of having an allergy to study treatments or its/their excipients, to opioids/opiates, muscle relaxants or their excipients, or other medication(s) used during general anesthesia.
  • Is expected to require mechanical ventilation after the procedure.
  • Has received or is planned to receive toremifene and/or fusidic acid via IV administration within 24 hours before or within 24 hours after administration of study treatment.
  • Use of medication expected to interfere with study treatments given in this trial.
  • Has been previously treated with sugammadex or has participated in a sugammadex clinical trial within 30 days of signing the informed consent form of this current trial.
  • Is currently participating in or has participated in an interventional clinical trial with an investigational compound or device within 30 days of signing the informed consent/assent for this current trial.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Part B. NeostigmineNeostigmine + GlycopyrrolateParticipants received a single IV bolus containing neostigmine (50 μg/kg; up to 5 mg maximum dose) in combination with either glycopyrrolate (10 μg/kg) or atropine sulfate (20 μg/kg) based on availability and/or contraindications, for moderate NMB reversal.
Part B. NeostigmineNeostigmine + AtropineParticipants received a single IV bolus containing neostigmine (50 μg/kg; up to 5 mg maximum dose) in combination with either glycopyrrolate (10 μg/kg) or atropine sulfate (20 μg/kg) based on availability and/or contraindications, for moderate NMB reversal.
Part A. Sugammadex 2 mg/kgSugammadex 2 mg/kgParticipants received a single intravenous (IV) bolus of sugammadex at 2 mg/kg for moderate NMB reversal.
Part A. Sugammadex 4 mg/kgSugammadex 4 mg/kgParticipants received a single IV bolus of sugammadex at 4 mg/kg for deep NMB reversal.
Part B. Sugammadex 2 mg/kgSugammadex 2 mg/kgParticipants received a single IV bolus of sugammadex at 2 mg/kg for moderate NMB reversal.
Part B. Sugammadex 4 mg/kgSugammadex 4 mg/kgParticipants received a single IV bolus of sugammadex at 4 mg/kg for deep NMB reversal.
Primary Outcome Measures
NameTimeMethod
Part A: Area Under the Plasma Concentration Time Curve From Time Zero to Infinity (AUC0-inf) for SugammadexDay 1: 2, 15, 30, 60, 240 to 360, and 600 to 720 minutes post-dose

Pharmacokinetic (PK) blood samples were collected in Part A from pediatric participants at multiple collection times post administration of sugammadex using a sparse sampling approach and used to determine AUC0-inf for sugammadex. As pre-specified by the Statistical Analysis Plan (SAP) for the PK analysis, all PK parameters were analyzed and reported by Part A age cohort (birth to \<27 days, 28 days to \<3 months, 3 to \<6 months, and 6 months to \< 2 years) for each dose (2 mg and 4 mg).

Part A: Area Under the Plasma Concentration Time Curve up to the Interpolated Concentration at 1 Hour Post Dose (AUC0-1hr) for SugammadexDay 1: 2, 15, 30, and 60 minutes (1 hour) post-dose

PK blood samples were collected in Part A from pediatric participants at multiple collection times post administration of sugammadex using a sparse sampling approach and used to determine AUC0-1hr for sugammadex. As pre-specified by the SAP for the PK analysis, all PK parameters were analyzed and reported by Part A age cohort (birth to \<27 days, 28 days to \<3 months, 3 to \<6 months, and 6 months to \< 2 years) for each dose (2 mg and 4 mg).

Part A: Area Under the Plasma Concentration Time Curve up to the Interpolated Concentration at 4 Hours Post Dose (AUC0-4hr) for SugammadexDay 1: 2, 15, 30, 60, and 240 minutes (4 hours) post-dose

PK blood samples were collected in Part A from pediatric participants at multiple collection times post administration of sugammadex using a sparse sampling approach and used to determine AUC0-4hr for sugammadex. As pre-specified by the SAP for the PK analysis, all PK parameters were analyzed and reported by Part A age cohort (birth to \<27 days, 28 days to \<3 months, 3 to \<6 months, and 6 months to \< 2 years) for each dose (2 mg and 4 mg).

Part A: Maximum Plasma Concentration (Cmax) of SugammadexDay 1: 2, 15, 30, 60, 240 to 360, and 600 to 720 minutes post-dose

PK blood samples were collected in Part A from pediatric participants at multiple collection times post administration of sugammadex using a sparse sampling approach and used to determine Cmax for sugammadex. As pre-specified by the SAP for the PK analysis, all PK parameters were analyzed and reported by Part A age cohort (birth to \<27 days, 28 days to \<3 months, 3 to \<6 months, and 6 months to \< 2 years) for each dose (2 mg and 4 mg).

Part A: Plasma Clearance (CL) of SugammadexDay 1: 2, 15, 30, 60, 240 to 360, and 600 to 720 minutes post-dose

PK blood samples were collected in Part A from pediatric participants at multiple collection times post administration of sugammadex using a sparse sampling approach and used to determine CL for sugammadex. As pre-specified by the SAP for the PK analysis, all PK parameters were analyzed and reported by Part A age cohort (birth to \<27 days, 28 days to \<3 months, 3 to \<6 months, and 6 months to \< 2 years) for each dose (2 mg and 4 mg).

Part A: Apparent Volume of Distribution (Vd) for SugammadexDay 1: 2, 15, 30, 60, 240 to 360, and 600 to 720 minutes post-dose

PK blood samples were collected in Part A from pediatric participants at multiple collection times post administration of sugammadex using a sparse sampling approach and used to determine Vd for sugammadex. As pre-specified by the SAP for the PK analysis, all PK parameters were analyzed and reported by Part A age cohort (birth to \<27 days, 28 days to \<3 months, 3 to \<6 months, and 6 months to \< 2 years) for each dose (2 mg and 4 mg).

Apparent Volume of Distribution at Steady State (Vss) for SugammadexDay 1: 2, 15, 30, 60, 240 to 360, and 600 to 720 minutes post-dose

PK blood samples were collected in Part A from pediatric participants at multiple collection times post administration of sugammadex using a sparse sampling approach and used to determine Vss for sugammadex. As pre-specified by the SAP for the PK analysis, all PK parameters were analyzed and reported by Part A age cohort (birth to \<27 days, 28 days to \<3 months, 3 to \<6 months, and 6 months to \< 2 years) for each dose (2 mg and 4 mg).

Part A: Half-Life (t1/2) of Sugammadex in PlasmaDay 1: 2, 15, 30, 60, 240 to 360, and 600 to 720 minutes post-dose

PK blood samples were collected in Part A from pediatric participants at multiple collection times post administration of sugammadex using a sparse sampling approach and used to determine t½ for sugammadex. As pre-specified by the SAP for the PK analysis, all PK parameters were analyzed and reported by Part A age cohort (birth to \<27 days, 28 days to \<3 months, 3 to \<6 months, and 6 months to \< 2 years) for each dose (2 mg and 4 mg).

Part B: Time to Neuromuscular Recovery (TTNMR) In Reversal of Moderate BlockWithin Day 1

Time to neuromuscular recovery was defined as the interval from administration of reversal agent to time to neuromuscular recovery. TTNMR could be assessed by 1 of 4 methods selected by the investigator, based on their judgment of what was technically feasible and clinically appropriate for the participant's procedure. These methods were inclusive of both clinical signs (head lift or hip flexion) and neuromuscular transmission monitoring using either a standard peripheral nerve stimulator or the technically challenging quantitative neuromuscular monitoring to train-of-four (TOF) ratio ≥0.9. As pre-specified by the protocol and SAP, TTNMR was analyzed only in Part B participants under the setting of moderate block for comparison of sugammadex 2 mg to neostigmine.

Parts A and B: Percentage of Participants With Adverse Events (AEs) Up To 7 Days Post Administration of Study MedicationUp to Day 7

An AE was any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. As pre-specified by the protocol and SAP, the primary analysis of safety combined data across Part A and Part B (and across age cohorts) and included all AEs that occurred up to 7 days post administration of study medication. The percentage of participants with an AE was reported by treatment and dose received.

Secondary Outcome Measures
NameTimeMethod
Part B: Time to Extubation In Reversal of Moderate BlockWithin Day 1

Time to extubation was defined as the interval from administration of reversal agent to removal of the endotracheal tube. Monitoring of time to extubation during Part B (moderate block) was achieved using the Extubation Readiness Assessment, which evaluated and documented clinically relevant elements including neuromuscular recovery, mental status, return of spontaneous ventilation, adequate oxygenation, hemodynamically stabile, and core body temperature with "Yes"/"No" answers (no overall score or direction attributed). The Operating Room anesthesiologist or other trained personnel were responsible for assessing extubation readiness beginning about 1 minute after study treatment administration and reassessing every 60 seconds until time of extubation readiness was achieved. As pre-specified by the protocol, Time to Extubation was analyzed only in Part B under setting of moderate block, and Part A participants were not included in this analysis.

Trial Locations

Locations (39)

University Medical Center Groningen ( Site 4227)

🇳🇱

Groningen, Netherlands

Wilhelmina Kinderziekenhuis ( Site 4228)

🇳🇱

Utrecht, Netherlands

Variety Children's Hospital D.B.A. Nicklaus Children's Hospital ( Site 3019)

🇺🇸

Miami, Florida, United States

The Children's Hospital of Philadelphia ( Site 3021)

🇺🇸

Philadelphia, Pennsylvania, United States

University of Vermont Medical Center ( Site 3013)

🇺🇸

Burlington, Vermont, United States

Queensland Children s Hospital ( Site 3806)

🇦🇺

South Brisbane, Queensland, Australia

Lucille Packard Children's Hospital ( Site 3008)

🇺🇸

Palo Alto, California, United States

Instituto da Crianca do Hospital das Clinicas-FMUSP ( Site 3825)

🇧🇷

Sao Paulo, Brazil

Children's Hospital of Pittsburgh UPMC ( Site 3017)

🇺🇸

Pittsburgh, Pennsylvania, United States

C.H.R.U. de Lille. Hopital Jeanne de Flandres ( Site 3304)

🇫🇷

Lille, Nord, France

UZ Leuven - Campus Gasthuisberg ( Site 3202)

🇧🇪

Leuven, Vlaams-Brabant, Belgium

McGovern Medical School at UT Health/ Memorial Hermann ( Site 3014)

🇺🇸

Houston, Texas, United States

Szegedi Tudomanyegyetem ( Site 4201)

🇭🇺

Szeged, Csongrad, Hungary

Scientific Research Institute Complex Problems Cardiovascular Disease ( Site 4288)

🇷🇺

Kemerovo, Kemerovskaya Oblast, Russian Federation

Scientific-Research Clinical Pediatric Institution n.a. Veltischev ( Site 4276)

🇷🇺

Moscow, Moskva, Russian Federation

Universitaire Ziekenhuis Antwerpen - UZA ( Site 3200)

🇧🇪

Edegem, Antwerpen, Belgium

UZ Brussel ( Site 3201)

🇧🇪

Brussels, Bruxelles-Capitale, Region De, Belgium

Hospital Pequeno Principe ( Site 3826)

🇧🇷

Curitiba, Parana, Brazil

Rigshospitalet ( Site 3250)

🇩🇰

Copenhagen, Hovedstaden, Denmark

St.Petersburg State Pediatric Medical University ( Site 4281)

🇷🇺

Saint Petersburg, Sankt-Peterburg, Russian Federation

Children City Clinical Hospital 13 n.a N.F.Filatov ( Site 4285)

🇷🇺

Moscow, Moskva, Russian Federation

Children City Clinical Hospital #9 n.a. G.N.Speransky ( Site 4290)

🇷🇺

Moscow, Moskva, Russian Federation

NMRC Obstetrics Gynecology and Perinatology n.a. V.I. Kulakov ( Site 4287)

🇷🇺

Moscow, Moskva, Russian Federation

Hospital Tacchini ( Site 3827)

🇧🇷

Bento Goncalves, Rio Grande Do Sul, Brazil

Instituto Nacional Cardiovascular Incor ( Site 3928)

🇵🇪

Lima, Peru

Hospital General de Zona No. 1 ( Site 4153)

🇲🇽

Villa De Alvarez, Colima, Mexico

New Childrens Hospital ( Site 3750)

🇫🇮

Helsinki, Uusimaa, Finland

Women and Children Hospital Kuala Lumpur (Hospital Tunku Azizah) ( Site 3875)

🇲🇾

Kuala Lumpur, Malaysia

Unidad de Cirugía Cardiovascular ( Site 4126)

🇬🇹

Guatemala, Guatemala

Debreceni Egyetem Klinikai Kozpont ( Site 4200)

🇭🇺

Debrecen, Hungary

University Malaya Medical Centre. ( Site 3876)

🇲🇾

Kuala Lumpur, Malaysia

Radboud University Medical Center ( Site 4226)

🇳🇱

Nijmegen, Gelderland, Netherlands

The Children s Hospital at Westmead ( Site 3805)

🇦🇺

Westmead, New South Wales, Australia

Sarawak General Hospital ( Site 3877)

🇲🇾

Kuching, Sarawak, Malaysia

Centenario Hospital Miguel Hidalgo-Pediatrics Department ( Site 4152)

🇲🇽

Aguascalientes, Mexico

Erasmus University Medical Center ( Site 4225)

🇳🇱

Rotterdam, Zuid-Holland, Netherlands

Pediatric Hematology Oncology and Immunology Centre n.a. D.Rogachev. ( Site 4275)

🇷🇺

Moscow, Moskva, Russian Federation

Royal Childrens Hospital Melbourne ( Site 3801)

🇦🇺

Parkville, Victoria, Australia

OU Medical Center ( Site 3005)

🇺🇸

Oklahoma City, Oklahoma, United States

© Copyright 2025. All Rights Reserved by MedPath