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Cladribine

Phase 1

Multiple Sclerosis | Small molecule | Neurology |Merck KGaA|Last Updated: Mar 15, 2024

Success Probability

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Trial Design

RandomizedCONTROLLED
Total Trials1
Total Enrollment18

FDA Designations

No designations recorded

Clinical trial landscape

Cladribine · 2 trials · 2 indications

Phase 1 2
NCT03745144Effects of Cladribine Tablets on the PK of Microgynon®Relapsing Multiple Sclerosis (RMS)
COMPLETED28 Analytics
NCT00938366Drug-Drug Interaction of Cladribine and Pantoprazole in Multiple Sclerosis SubjectsMultiple Sclerosis
COMPLETED18 Analytics
PHASE1COMPLETED
Effects of Cladribine Tablets on the PK of Microgynon®
Relapsing Multiple Sclerosis (RMS)Unlock trial analytics
PHASE1COMPLETED
Drug-Drug Interaction of Cladribine and Pantoprazole in Multiple Sclerosis Subjects
Multiple SclerosisUnlock trial analytics

Study Endpoints

Primary Endpoints

Area Under the Plasma Concentration-Time Curve From Zero to Tau at Steady State (AUCt,ss) of Ethinyl Estradiol and Levonorgestrel
Pre-dose, 0.5, 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 14

Area under the plasma concentration-time curve from zero to tau at steady state (AUCt,ss) of ethinyl estradiol and levonorgestrel were reported. Calculated using descriptive statistics.

Maximum Observed Plasma Concentration in Steady State (Cmax,ss) of Ethinyl Estradiol And Levonorgestrel
Pre-dose, 0.5, 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 14

Maximum observed plasma concentration in steady state (Cmax,ss) of ethinyl estradiol and levonorgestrel were reported. Calculated using descriptive statistics.

Minimum Observed Plasma Concentration in Steady State (Cmin,ss) of Ethinyl Estradiol and Levonorgestrel
Pre-dose, 0.5, 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 14

Minimum observed plasma concentration in steady state (Cmin,ss) of ethinyl estradiol and levonorgestrel were reported. Calculated from descriptive statistics.

Plasma Concentration at End of Dosing Interval at Steady State (Ctrough) of Ethinyl Estradiol and Levonorgestrel
Pre-dose, 0.5, 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 14

Plasma concentration at end of dosing interval at steady state (Ctrough) of ethinyl estradiol and levonorgestrel were reported. Calculated from descriptive statistics.

Time to Reach the Maximum Observed Plasma Concentration At Steady State (Tmax,ss) of Ethinyl Estradiol and Levonorgestrel
Pre-dose, 0.5, 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 14

Time to reach the maximum observed plasma concentration at steady state (Tmax,ss) of Ethinyl Estradiol and Levonorgestrel were reported. Calculated using descriptive statistics.

Average Plasma Concentration at Steady State (Cav,ss) of Ethinyl Estradiol and Levonorgestrel
Pre-dose, 0.5, 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 14

Average plasma concentration at steady state (Cav,ss) ) of Ethinyl Estradiol and Levonorgestrel were reported. Cav,ss =AUCt,ss/ tau, where, AUCt,ss was defined as the area under the plasma concentration-time curve in steady state during a complete dosing interval (tau) and Tau is the Complete dosing interval. Calculated using descriptive statistics.

Peak-to-Trough Fluctuation Over One Complete Dosing Interval At Steady State (PTF%)
Pre-dose, 0.5, 1, 2, 4, 6, 8, 12 and 24 hours post-dose on Day 14

The PTF within complete dosing interval at steady state, calculated as PTF (%) = (\[Cmax - Cmin\]/Cav) multiplied by 100. Here, Cmin means the minimum plasma concentration, Cmax means the maximum plasma concentration and Cav means the average plasma concentration of drug and metabolite.

Maximum Plasma Concentration (Cmax) of Cladribine
Pre-dose (within 30 minutes prior to dosing) and at 0.5,1, 3, 6, 8, 12,16, 24, 36, 48 Hour post-dose

The maximum or peak plasma concentration observed after the administration of cladribine.

Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC0-inf) of Cladribine
Pre-dose (within 30 minutes prior to dosing) and at 0.5,1, 3, 6, 8, 12,16, 24, 36, 48 Hour post-dose

The AUC(0-inf) was estimated by determining the total area under the curve of the concentration versus time curve extrapolated to infinity.

Secondary Endpoints

Number of Participants With Treatment -Emergent Adverse Events (TEAEs)
Up to Day 84
Number of Participants With Clinically Relevant Change From Baseline in Laboratory Values
Up to Day 84
Number of Participants With Clinically Relevant Change From Baseline in Electrocardiogram (ECG)
Up to Day 84
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelCROSSOVER
PurposeOTHER

Treatment Arms

ArmTypeDescription
Sequence 1: First Cladribine, Then PlaceboEXPERIMENTALPeriod 1: Participants received a single once daily dose of Microgynon® tablet from Day 1-8 followed by 5-day once-daily Cladribine 10 to 20 milligram(mg) depending on body weight along with Microgynon® tablet once daily from Day 9-28. Period 2: Participants received a single once daily dose of Microgynon® tablet from Day 1-8 followed by 5-day once-daily Cladribine matched Placebo along with Microgynon® from Day 9-14. From Day 15-28 participants received once daily Microgynon® along with 5-day once-daily Cladribine 10 to 20 mg depending on body weight.
Sequence 2: First Placebo, Then CladribineEXPERIMENTALParticipants 5-day once daily Period 1: Participants received a single once daily dose of Microgynon® tablet from Day 1-8 followed by 5-day once-daily Cladribine matched Placebo along with Microgynon® tablet once daily from Day 9-28. Period 2: Participants received a single once daily dose of Microgynon® tablet from Day 1-8 followed by 5-day once-daily Cladribine 10 to 20 mg depending on body weight along with Microgynon® tablet once daily from Day 9-28.
Microgynon®EXPERIMENTALParticipants received Microgynon® for 21 days, starting on the first day of the menstrual cycle.
Cladribine followed by Cladribine + PantoprazoleEXPERIMENTALSubjects will receive a single dose of cladribine10 milligram (mg) orally on Day 1. After a wash out period of 10-25 days, subjects will receive pantoprazole 40 mg orally for 2 consecutive days. On Day 2 of the pantoprazole administration, a single dose of cladribine 10 mg will be administered orally 3 hours after the second pantoprazole dose.
Cladribine + pantoprazole followed by CladribineEXPERIMENTALSubjects will receive pantoprazole 40 mg orally for 2 consecutive days. On Day 2 of the pantoprazole administration, a single dose of cladribine 10 mg will be administered orally 3 hours after the second pantoprazole dose. After a wash out period of 10-25 days, subjects will receive a single dose of cladribine 10 mg orally.

Interventions

NameTypeDescription
CladribineDRUGParticipants received cladribine once-daily for 5 consecutive days in treatment period 1 and 2.
PlaceboDRUGParticipants received placebo matched to cladribine once-daily for 5 consecutive days in treatment period 1 and 2.
Microgynon®DRUGParticipants received Microgynon® tablet once daily for 21 days in treatment period 1 and 2. Participants received Microgynon® for 21 days, starting on the first day of the menstrual cycle in Run-in period.
PantoprazoleDRUGSubjects will receive a pantoprazole 40 mg orally for 2 consecutive days either in first or second intervention period.
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Eligibility Criteria

Age Range18 Years to 45 Years
SexFEMALE
Healthy VolunteersNo
Study Sites7

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) * A...

Countries:GermanyPoland
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Frequently asked questions about Cladribine

What is Cladribine used for in Multiple Sclerosis?

Cladribine is a small molecule being developed by Merck KGaA for the treatment of Multiple Sclerosis, including Relapsing Multiple Sclerosis (RMS). It is currently in Phase 1 clinical development for these neurological conditions.

Who makes Cladribine?

Cladribine is developed by Merck KGaA, a company traded under the ticker MKGAF. The drug is being studied as a treatment for Multiple Sclerosis and Relapsing Multiple Sclerosis.

What phase is Cladribine in?

Cladribine is in Phase 1 clinical development. It is an investigational drug for Multiple Sclerosis and Relapsing Multiple Sclerosis, and it is not yet approved for these indications.

What clinical trials is Cladribine in?

Cladribine has been studied in two completed Phase 1 trials. One trial, NCT00938366, examined drug-drug interactions with pantoprazole in Multiple Sclerosis subjects. Another trial, NCT03745144, studied the effects of Cladribine tablets on the pharmacokinetics of Microgynon in Relapsing Multiple Sclerosis patients.

Is Cladribine the same as Mavenclad?

Cladribine is the active ingredient in the product Mavenclad, which is used for treating relapsing forms of multiple sclerosis. The clinical trials listed for Cladribine tablets are part of its development for Multiple Sclerosis and Relapsing Multiple Sclerosis.