Phase 1
Completed N=28
Effects of Cladribine Tablets on the PK of Microgynon®
Relapsing Multiple Sclerosis (RMS)
Source: ClinicalTrials.gov NCT03745144 ↗
Enrolled (actual)
28
Serious AEs
0.0%
Results posted
Mar 2024
Primary outcomePrimary: Area Under the Plasma Concentration-Time Curve From Zero to Tau at Steady State (AUCt,ss) of Ethinyl Estradiol and Levonorgestrel — 789; 817; 91400; 92000 hour*picograms per millilitre(h*pg/ml)
Summary
The purpose of this study was to investigate the potential effects of cladribine on the pharmacokinetics (PK) of monophasic oral contraceptive microgynon® by assessment of its constituents, ethinyl estradiol (EE) and levonorgestrel (LNG).
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Plasma Concentration-Time Curve From Zero to Tau at Steady State (AUCt,ss) of Ethinyl Estradiol and Levonorgestrel |
789; 817; 91400; 92000 | — |
| PRIMARY Maximum Observed Plasma Concentration in Steady State (Cmax,ss) of Ethinyl Estradiol And Levonorgestrel |
88.3; 88.1; 7950; 8150 | — |
| PRIMARY Minimum Observed Plasma Concentration in Steady State (Cmin,ss) of Ethinyl Estradiol and Levonorgestrel |
14.8; 14.7; 2520; 2430 | — |
| PRIMARY Plasma Concentration at End of Dosing Interval at Steady State (Ctrough) of Ethinyl Estradiol and Levonorgestrel |
15.5; 15.4; 2580; 2580 | — |
| PRIMARY Time to Reach the Maximum Observed Plasma Concentration At Steady State (Tmax,ss) of Ethinyl Estradiol and Levonorgestrel |
1.00; 1.00; 1.00; 1.00 | — |
| PRIMARY Average Plasma Concentration at Steady State (Cav,ss) of Ethinyl Estradiol and Levonorgestrel |
32.9; 34.1; 3810; 3830 | — |
| PRIMARY Peak-to-Trough Fluctuation Over One Complete Dosing Interval At Steady State (PTF%) |
220; 213; 140; 145 | — |
| SECONDARY Number of Participants With Treatment -Emergent Adverse Events (TEAEs) |
7; 3; 9; 5; 5; 4 | — |
| SECONDARY Number of Participants With Clinically Relevant Change From Baseline in Laboratory Values |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Relevant Change From Baseline in Electrocardiogram (ECG) |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Relevant Change From Baseline in Vital Signs |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Maximum Plasma Concentration (Cmax) of Cladribine |
29.3; 28.2; 23.6; 22.7 | — |
| SECONDARY Time to Reach the Maximum Observed Plasma Concentration (Tmax) of Cladribine |
0.500; 0.500; 0.500; 0.500 | — |
Eligibility Criteria
Inclusion Criteria
- Are pre-menopausal women with or without child-bearing potential with a negative serum pregnancy test, and women with child-bearing potential receiving adequate birth control
- Participants with diagnosis of clinically stable and definite relapsing multiple sclerosis (RMS)
- Adequate hematological, hepatic and renal function as defined in the protocol
- Are able and willing to accept dietary restrictions and restrictions regarding the use of concomitant medications (including over-the-counter products, herbal medicines and dietary supplements) over the course of the study
- Had a body weight and body mass index (BMI) within the range at screening
- Other protocol defined inclusion criteria could apply
Exclusion Criteria
- History of clinically relevant allergy or known hypersensitivity to the active substance or to any of the excipients of cladribine tablets or hypersensitivity to drugs with a similar chemical structure to cladribine - History of clinically relevant allergy or known hypersensitivity to 1 of the active substances levonorgestrel (LNG) or ethinylestradiol (EE) or to any excipients of Microgynon® tablets
- Positive results from serology examination for Hepatitis B surface antigen (HbsAg) not due to vaccination, hepatitis B core antibody (HbcAb), Hepatitis C virus antibody (anti- HCV) or Human Immunodeficiency antibody (anti-HIV)
- Presence or risk of venous thromboembolism (VTE) arterial thromboembolism (ATE)
- Diabetes mellitus (Type 1 or Type 2) with vascular manifestations
- Signs or symptoms of neurological disease other than multiple sclerosis (MS) that could explain the symptoms of the participant
- Presence of gastrointestinal (GI) disease or history of gastrointestinal -tract surgery
- Exposure to another investigational drug within the last 2 months or within last 6 month if agent is known to be immunosuppressive
- Other protocol defined exclusion criteria could apply
Data sourced from ClinicalTrials.gov (NCT03745144). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.