A Study of Pharmacokinetics, Safety and Tolerability of Dimolegin (DD217)

NCT05181241 | Completed Phase 1

• 1 other identifier: KI-01-2016
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

In the course of the clinical study, the pharmacokinetics, pharmacodynamics, safety and tolerability of Dimolegin (DD217) 10 mg enteric-coated tablets after single administration to healthy volunteers at increasing doses were studied. 24 volunteers participated in the study. The randomization procedure was carried out for 24 volunteers selected at screening. In Group 1 6 volunteers were randomized , in Group 2 6 volunteers were randomized, and in Group 3 12 volunteers were enrolled. Group 1 volunteers took the study drug at a dose of 20 mg once, group 2 volunteers took the study drug at a dose of 40 mg once, and group 3 volunteers took the study drug at a dose of 60 mg once.

Conditions

Healthy Volunteers

Keywords

Dimolegin; Dioxaban; DD217; Factor Xa Inhibitor; anticoagulant; therapeutic anticoagulation; thromboprophylaxis; anticoagulation; healthy

Outcome Measures

Primary Outcomes (1)

• Total Adverse Events (AE)

  Number of of subjects experiencing AEs, serious adverse events (SAEs), or discontinuations due to AEs

  28 Days

Secondary Outcomes (8)

• The increase in Anti-Xa activity

  2 Days

• The increase in International Normalised Ratio (INR)

  2 Days

• The increase in Activated Partial Thromboplastin Time (aPTT)

  2 Days

• Steady-state Area Under the Plasma Concentration Versus Time Curve From Time Zero to 12 Hours of Dioxaban (AUC (0-12))

  7 Days

• Steady state Elimination of Half-Life of Dioxaban (t½)

  7 Days

Study Arms (3)

Group No. 1 (n=6) Dimolegin - 20 mg

EXPERIMENTAL

Group No. 1 (n=6) consisted of 2 cohorts with 3 volunteers per each. Volunteers of Cohorts 1 and 2 received Dimolegin (DD217) once at a dose of 20 mg

Drug: Dimolegin

Group No. 2 (n=6) Dimolegin - 40 mg

EXPERIMENTAL

Group No. 2 (n=6) consisted of 2 cohorts with 3 volunteers per each. Volunteers of Cohorts 3 and 4 received Dimolegin (DD217) once at a dose of 40 mg

Drug: Dimolegin

Group No. 3 (n=12) Dimolegin - 60 mg

EXPERIMENTAL

Group No. 3 (n=12) consisted of 3 cohorts. Cohorts 5 and 6 included 3 volunteers per each, and Cohort 7 included 6 volunteers. All Group 3 volunteers received Dimolegin (DD217) once at a dose of 60 mg

Drug: Dimolegin

Interventions

Dimolegin DRUG

Dimolegin (DD217) - enteric coated tablets 10 mg developed by PharmaDiall Ltd (Moscow), manufactured by Federal State Unitary Enterprise Research and Practical Center "Pharmaceutical Protection" at The Federal Medical Biological Agency (FMBA) of Russia

Also known as: DD217

Group No. 1 (n=6) Dimolegin - 20 mg; Group No. 2 (n=6) Dimolegin - 40 mg; Group No. 3 (n=12) Dimolegin - 60 mg

Eligibility Criteria

• Age: 18 Years - 45 Years
• Gender Eligibility Details: Male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Male
• years
• Verified "healthy" diagnosis based on the findings of routine clinical, laboratory, and instrumental examinations
• Body mass index (BMI) is 18.5-30.0 kg/m2
• Consent to the use of barrier contraception methods during the study period and for 3 months after it
• Written consent of the volunteer to enrollment

You may not qualify if:

• Aggravated allergy history
• Drug intolerance
• Acute and chronic cardiovascular, bronchopulmonary, neuroendocrine diseases as well as gastrointestinal, hepatic, renal, hematological diseases
• Systolic blood pressure less than 90 mmHg or above 130 mmHg
• Diastolic blood pressure less than 70 mmHg or above 89 mmHg
• Pulse rate less than 60 bpm or more than 89 bpm
• Gastrointestinal surgery (except for appendectomy)
• Acute infectious diseases less than 4 weeks prior to the study
• Any abnormalities detected during screening from the clinical laboratory center reference values (including estimated glomerular filtration rate (GFR), coagulation profile), clinical and instrumental study methods
• Hypersensitivity to the study product components
• Taking prescription or over-the-counter medications, including dietary supplements, herbal products, vitamins, homeopathic medicines, less than 2 weeks before the start of the study
• Administration of medicinal products with expressed effect on hemodynamics, hepatic function and other systems (e.g. barbiturates, omeprazole, cimetidine, etc.) less than 2 months prior to the study initiation
• Blood donation (≥ 450 mL of blood or plasma) less than 2 months prior to the study
• Participation in clinical studies of drug products less than 3 weeks prior to the study initiation
• Intake of more than 10 units of alcohol per week (10 mL of pure (100 %) ethanol is taken for 1 unit of alcohol, this is the amount that the body of a healthy adult breaks down within an hour; 1 unit of alcohol is equivalent to 0.33 liters of beer, 150 mL of wine or 30 mL of hard liquors), or history of alcohol or drug dependence, drug abuse

Sponsors & Collaborators

• PharmaDiall Ltd.: lead

Study Sites (1)

Non-Governmental Private Healthcare Institution of Sci-entific Clinical Center of Russian Railways JSC

Moscow, 125315, Russia

Location

Related Publications (2)

• Tovbin DG, Tarasov DN, Malakhov DV, Tserkovnikova NA, Aybush AV, Drozd NN. The Development of New Low-Molecular-Weight Factor Xa Inhibitors that are Potential Anticoagulants. Curr Drug Discov Technol. 2022;19(1):e010921191770. doi: 10.2174/1568009621666210224104940.

  PMID: 33655836 BACKGROUND

• Tarasov DN, Tovbin DG, Malakhov DV, Aybush AV, Tserkovnikova NA, Savelyeva MI, Sychev DA, Drozd NN, Savchenko AY. The Development of New Factor Xa Inhibitors Based on Amide Synthesis. Curr Drug Discov Technol. 2018;15(4):335-350. doi: 10.2174/1570163815666180215114732.

  PMID: 29468977 BACKGROUND

MeSH Terms

Interventions

(+-)-(1'R*,2'S*,6'R*)-(2-hydroxy-4,6-dimethoxyphenyl)(3'-methyl-2'-(3''-methylbut-2''-enyl)-6-phenylcyclohex-3'-enyl)methanone

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Model Details: The study is single center, open-label, prospective, non-randomized with sequential enrollment of volunteers with dose escalation

Study Record Dates

• First Submitted: December 3, 2021
• First Posted: January 6, 2022
• Study Start: January 25, 2017
• Primary Completion: December 25, 2017
• Study Completion: April 25, 2018
• Last Updated: January 6, 2022

Record last verified: 2021-12

Data Sharing

• IPD Sharing: Will not share

Locations

RU (1)