Phase 1 Clinical Study to Describe Biological Safety and Pharmacokinetics of Tyrphostin

Phase 1 Clinical Study To Describe the Biological Safety and Pharmacokinetics of Tyrphostin AG-17 Present in Oral Solid Formulations of the Fixed Dose Combination, in Three Different Concentrations of the Compound Tyrphostin AG-17 Content 10 mg, 3.3 mg and 1 mg Respectively, With 700 mg of L-Carnitine Tartrate Each Presentation, in a Single Dose in Healthy Research Subjects of Mexican Nationality

Evaluate the biological safety and pharmacokinetics of tyrphostin AG-17 present in the solid oral formulations of the fixed-dose combination, in three different concentrations of the compound tyrphostin AG-17 contained 10 mg, 3.3 mg and 1 mg, respectively, with 700 mg of L-Carnitine tartrate each presentation, in a single dose in healthy research subjects of Mexican nationality.

Study Overview

• Status: Enrolling by invitation
• Conditions: Healthy
• Intervention / Treatment: Combination product: Tirfostina/L-Carnitina

Detailed Description

Describe the tolerance of the fixed-dose combination, in three different concentrations of the compound tyrphostin AG-17, containing 10 mg, 3.3 mg and 1 mg, respectively, with 700 mg of L-Carnitine tartrate each presentation, in a single dose in research subjects. healthy Mexican nationals, describing: type, frequency, duration, consequence, relationship with clinical history, management, follow-up; criteria: seriousness, severity; and classification of the AE or ADRs in accordance with the current NOM-220-SSA1 and estimate if there are differences by gender.

Assess the effects on body functions of the fixed dose combination, in three different concentrations of the compound tyrphostin AG-17 content 10 mg, 3.3 mg and 1 mg respectively, with 700 mg of L-Carnitine tartrate each presentation, in a single dose in healthy research subjects of Mexican nationality through the measurement of physiological markers and estimate if there are differences by gender.

Obtain the biological blood samples necessary for the quantification of the compound tyrphostin AG-17 in concentrations of 10 mg, 3.3 mg and 1 mg in accordance with Good Clinical Practices, always taking care to protect the vulnerability and integrity of the research subjects.

Quantifying the compound tyrphostin AG-17 with a previously validated bioanalytical method.

Estimate the pharmacokinetic parameters of the compound tyrphostin AG-17 at concentrations of 10 mg, 3.3 mg and 1 mg.

Describe the pharmacokinetic parameters of the compound tyrphostin AG-17 in concentrations of 10 mg, 3.3 mg and 1 mg in terms of Cmax, AUC0-t, AUC0-inf and as secondary parameters AUCExt, TMR, Tmax, Ke, t½, Vd and CL and estimate if there are differences by gender.

Establish the possible linearity of the compound tyrphostin AG-17 in concentrations of 10 mg, 3.3 mg and 1 mg.

Correlate the pharmacokinetic markers with the presence of AE or ADRs, with the hemodynamic markers and with the physiological markers and present a dynamic profile of the compound under investigation to propose a pharmacological response that is of potential further interest.

• Study Type: Interventional
• Enrollment (Anticipated): 48
• Phase: Early Phase 1

Contacts and Locations

Study Locations

• Mexico
  • Azcapotzalco
    • Ciudad de México, Azcapotzalco, Mexico, 02230
      • Pharmet, S.A de C.V.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 16 years to 53 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Research subjects aged: between 18 and 55 years.
• Sex: 24 men and 24 women.
• Weight: Research subjects with Body Mass Index between 18-27 kg/m2.
• Research subjects with a diagnosis of "HEALTHY"; For this, a clinical history, medical examination, physical examination will be carried out in addition to taking samples to perform clinical analyzes (complete blood count with differential count, to evaluate hematological function, blood chemistry that evaluates pancreatic, renal, hepatic function, cardiac risk, metabolic function, biosafety tests, studies to rule out the presence of hepatitis B and C, HIV and VDRL, general urine test, fasting,). The results of the laboratory tests will be reviewed according to the reference values given by the laboratory and/or the reference values of Instruction I-DCL-VAL-030 "Range of normal values of laboratory tests", the tests The biosafety tests will have to have a NON-REACTIVE result and the cabinet studies (ECG) will have to have a NORMAL diagnosis granted by the Pharmometrica medical staff that evaluates them.
• Research subjects with NEGATIVE results on qualitative drug of abuse tests, breathalyzer and rapid urine pregnancy test (for females), at the beginning of the study.
• Based on the foregoing, the medical staff will determine whether the research subject has the physical capacity to participate in the study. Healthy will be understood as the research subject that meets all the inclusion criteria and does not meet any exclusion criteria.
• Signature of the informed consent for participation in this study, by the IS.

Exclusion Criteria:

• Research subjects with a medical history of allergies.
• Research subjects who have ingested alcoholic beverages, tobacco or xanthines within 48 hours prior to the study.
• Research subjects who have consumed grapefruit, grape, strawberry juice (generally red fruits such as blackberries or blueberries), spicy or charcoal-cooked foods 72 h prior to the study.
• Research subjects who have participated in clinical research studies of any molecule, within 3 months prior to the study date.
• Research subjects who were hospitalized for any reason or were seriously ill within 60 days prior to the study.
• Research subjects who have donated or lost 450 mL or more of blood within 45 days prior to the study.
• Research subjects with disease that require the use of medications Research subjects with medical history of cardiovascular, gastrointestinal, hepatic and/or renal insufficiency.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Single Group Assignment
• Masking: Double

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Group 1; Tyrphostin AG-17 content 10 mg with 700 mg of L-Carnitine tartrate	Combination product: Tirfostina/L-Carnitina; Estudio clínico fase 1 para describir la seguridad biológica y la farmacocinética de la tirfostina AG-17
Experimental: Group 2; Tyrphostin AG-17 content 3.3 mg with 700 mg of L-Carnitine tartrate	Combination product: Tirfostina/L-Carnitina; Estudio clínico fase 1 para describir la seguridad biológica y la farmacocinética de la tirfostina AG-17
Experimental: Group 3; Tyrphostin AG-17 content 1 mg with 700 mg of L-Carnitine tartrate	Combination product: Tirfostina/L-Carnitina; Estudio clínico fase 1 para describir la seguridad biológica y la farmacocinética de la tirfostina AG-17

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Tolerance assessment	Description: type, frequency, duration, consequence, relationship with clinical history, management, follow-up; Criteria: severity (serious [serious] and non-serious), severity (mild, moderate and severe); Classification: certain, likely, possible, unlikely, conditional/unclassified, not evaluable/unclassifiable	30 days

Collaborators and Investigators

• Sponsor: Molecule X LLC

Study record dates

Study Major Dates

• Study Start (Actual): May 24, 2022
• Primary Completion (Actual): June 28, 2022
• Study Completion (Anticipated): July 29, 2022

Study Registration Dates

• First Submitted: March 1, 2022
• First Submitted That Met QC Criteria: August 2, 2022
• First Posted (Actual): August 4, 2022

Study Record Updates

• Last Update Posted (Actual): August 4, 2022
• Last Update Submitted That Met QC Criteria: August 2, 2022
• Last Verified: August 1, 2022

More Information

Terms related to this study

• Keywords: Pharmacokinetics; L-Carnitine; Phase 1 clinical study; Tirfostin; Biological Safety
• Other Study ID Numbers: F1-TIR-036/0821

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: No
• IPD Plan Description: The blood samples obtained as a result of this study will be used to describe a possible change and/or damage in the organism and for the quantification of tyrphostin AG-17, as well as all the data obtained by this research will be evaluated maintaining its confidentiality, adjusting its compliance with the Federal Law on Protection of Personal Data Held by Private Parties

Drug and device information, study documents

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