First in Human Study to Compare Safety Between Intravenous Bolus Versus Infusion of ApTOLL (APTABOLUS)

First in Human Clinical Trial to Compare Safety and Tolerability Between Intravenous Infusions and Bolus Intravenous Inhection of ApTOLL in Healthy Volunteers

The main objective of the study is to assess the tolerability and safety of ApTOLL administration when comparing intravenous infusion vs. bolus intravenous injection, in healthy volunteers. Pharmacokinetic profile of ApTOLL will be also analysed as secondary objective of the study.

Study Overview

• Status: Completed
• Conditions: Stroke
• Intervention / Treatment: Drug: ApTOLL

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• Spain
  • Madrid, Spain, 28006
    • Clinical Pharmacology Department. Hospital Universitario de La Princesa

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Male or female (with no possibility to become pregnant (hysterectomized or menopausal women)) subjects who give their written consent to participate in the study.
• Aged from 18 to 55.
• No clinically significant organic or psychic conditions.
• No clinically significant abnormalities in medical records and physical examination.
• No clinically significant abnormalities in haematology, coagulation, biochemistry, serology and urinalysis .
• No clinically significant abnormalities in vital signs and electrocardiogram.

Exclusion Criteria:

• Subjects affected by an organic or psychic condition.
• Subjects who have received prescribed pharmacological treatment in the last 15 days or any kind of medication in the 48 hours prior to receiving the study medication
• Subjects with body mass index (weight (kg)/height2 (m2)) outside the 18.5-30.0 range.
• History of sensitivity to any drug.
• Positive drug screening (for cannabis, opiates, cocaine and amphetamines).
• Smoker.
• Daily consumers of alcohol and/or acute alcohol poisoning in the last week.
• Having donated blood in the last month before start of the study.
• Participation in another study with administration of investigational drugs in the previous 3 months (if the study was conducted with drug substances marketed in Spain, a period of at least 1 month or 5 half lives, what is longer, will be considered).
• Inability to follow the instructions or collaborate during the study.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: ApTOLL treatment; Volunteers will receive a dose of ApTOLL of 0.1mg/kg administered intravenously as slow infusion one day and as a single bolus intravenous injection the second day. In a third and last admission day, volunteers will receive a dose of ApTOLL of 0.2mg/kg administered as a single bolus intravenous injection.	Drug: ApTOLL; ApTOLL will be administered as follows: Day 1: a dose of 0.1mg/kg will be administered intravenously as a slow infusion.; Day 2: a dose of 0.1mg/kg will be administered intravenously as single bolus injection.; Day 3: a dose of 0.2mg/kg will be administered intravenously as single bolus injection.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse Events	To evaluate the safety and tolerability between different ways of ApTOLL administration: intravenous infusion versus bolus intravenous injection, and pharmacokinetic characteristics of ApTOLL in healthy volunteers after single dose administration in fasting conditions.	day 1 to day 28

Collaborators and Investigators

• Sponsor: aptaTargets S.L.
• Collaborators: Centro para el Desarrollo Tecnológico Industrial
• Investigators: Study Director: Macarena Hernández, PhD, aptaTargets S.L.; Principal Investigator: Dolores Ochoa, MD, PhD, Hospital Universitario La Princesa

Publications and helpful links

General Publications

• Hernandez-Jimenez M, Martin-Vilchez S, Ochoa D, Mejia-Abril G, Roman M, Camargo-Mamani P, Luquero-Bueno S, Jilma B, Moro MA, Fernandez G, Pineiro D, Ribo M, Gonzalez VM, Lizasoain I, Abad-Santos F. First-in-human phase I clinical trial of a TLR4-binding DNA aptamer, ApTOLL: Safety and pharmacokinetics in healthy volunteers. Mol Ther Nucleic Acids. 2022 Mar 9;28:124-135. doi: 10.1016/j.omtn.2022.03.005. eCollection 2022 Jun 14.
• Fernández G, Moraga A, Cuartero MI, García-Culebras A, Peña-Martínez C, Pradillo JM, Hernández-Jiménez M, Sacristán S, Ayuso MI, Gonzalo-Gobernado R, Fernández-López D, Martín ME, Moro MA, González VM, Lizasoain I. TLR4-Binding DNA Aptamers Show a Protective Effect against Acute Stroke in Animal Models. Mol Ther. 2018 Aug 1;26(8):2047-2059. doi: 10.1016/j.ymthe.2018.05.019. Epub 2018 Jun 15.

Study record dates

Study Major Dates

• Study Start (Actual): April 25, 2022
• Primary Completion (Actual): June 24, 2022
• Study Completion (Actual): June 24, 2022

Study Registration Dates

• First Submitted: September 28, 2022
• First Submitted That Met QC Criteria: October 5, 2022
• First Posted (Actual): October 6, 2022

Study Record Updates

• Last Update Posted (Actual): October 6, 2022
• Last Update Submitted That Met QC Criteria: October 5, 2022
• Last Verified: October 1, 2022

More Information

Terms related to this study

• Other Study ID Numbers: APTABOLUS

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: Undecided
• IPD Plan Description: We have not planned this point yet

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No