Cladribine 10mg tablets
Requires a prescription from a doctor or prescriber
Drugs affecting the immune response
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Official medicine documents
Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Cladribine
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
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Suspected adverse reactions reported for Cladribine
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1 branded products available
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Mavenclad 10mg tablets
Therapeutically similar medicines
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Clinical guidelines and formulary information
British National Formulary
Cladribine
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(13)
Cladribine for treating relapsing–remitting multiple sclerosis (TA616)
Cladribine for treating active relapsing forms of multiple sclerosis (TA1053)
Avapritinib for treating advanced systemic mastocytosis (TA1012)
Natalizumab (originator and biosimilar) for treating highly active relapsing–remitting multiple sclerosis after disease-modifying therapy (TA1126)
Ponesimod for treating relapsing–remitting multiple sclerosis (TA767)
Ozanimod for treating relapsing–remitting multiple sclerosis (TA706)
Ofatumumab for treating relapsing multiple sclerosis (TA699)
Ocrelizumab for treating relapsing–remitting multiple sclerosis (TA533)
Midostaurin for treating advanced systemic mastocytosis (TA728)
Multiple sclerosis in adults: management (NG220)
Beta interferons and glatiramer acetate for treating multiple sclerosis (TA527)
icobrain ms for active relapsing–remitting multiple sclerosis (MIB291)
Ibrutinib for treating Waldenstrom's macroglobulinaemia (TA795)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Supply & product information
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
73 found
Half-life
2.5 hours
Mechanism
Heightened activity of B and T lymphocytes have been implicated in the pathophys…
Food interactions
1 warning
Human targets
12 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
40%
[L50688]
Following the oral administration of 10 mg cladribine, the mean maximum concentration (C…
Half-life
2.5 hours
Protein binding
20%
[L50693]
Protein binding is independent of concentration in vitro.
[L50688]
Volume of distribution
9 L/kg
[L50693]…
Metabolism
Elimination
18%
Clearance
0.12 mg/k
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
[L50693]
Oral cladribine is indicated for the treatment of relapsing forms of multiple sclerosis (MS), including relapsing-remitting disease and active secondary progressive disease, in adults. Because of its safety profile, the use of cladribine is generally recommended for patients who have had an inadequate response to, or are unable to tolerate, an alternate drug indicated for the treatment of MS.
[L50688][L50708]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 774 interactions
[L50698]
High doses of cladribine have been associated with irreversible neurologic toxicity (paraparesis/quadriparesis), acute nephrotoxicity, and severe bone marrow suppression resulting in neutropenia, anemia, and thrombocytopenia.
[L50693]
Lymphopenia may also occur, which is known to be dose-dependent.
[L50688]
There is no known antidote to cladribine overdosage; thus, treatment of overdosage consists of drug discontinuation, careful observation, and appropriate supportive measures.
[L50693]
Although it is not known whether cladribine can be removed from the circulation by dialysis or hemofiltration, because of its rapid and extensive intracellular and tissue distribution, hemodialysis is unlikely to eliminate cladribine to a significant extent.
[L50688]
Cladribine can also induce cytotoxicity via other mechanisms. It induces poly(ADP-ribose) polymerase (PARP), a DNA repair enzyme, that exhausts the intracellular levels of nicotinamide adenine dinucleotide (NAD) and adenosine triphosphate (ATP), thereby causing apoptotic cell death.[A350] Recent evidence shows that cladribine can trigger apoptosis by changing the mitochondrial transmembrane potential, allowing cytochrome c and apoptosis-inducing factor to move into the cytosol. This initiates apoptosis through both caspase-dependent and caspase-independent pathways.[A350]
Following oral administration, the lowest absolute lymphocyte counts occurred approximately 2 to 3 months after the start of each treatment cycle and were lower with each additional treatment cycle. At the end of Year 2, 2% of patients continued to have absolute lymphocyte counts less than 500 cells per microliter. The median time to recovery from lymphocyte counts less than 500 cells per microliter to at least 800 cells per microliter was approximately 28 weeks.[L50688]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[L50688]
Following the oral administration of 10 mg cladribine, the mean maximum concentration (Cmax) was in the range of 22 to 29 ng/ mL, and the corresponding mean AUC was in the range of 80 to 101 ng x h/mL.
[L50688]
The Cmax and AUC of cladribine increased proportionally across a dose range from 3 to 20 mg.
[L50688]
Under fasted conditions, the median time to maximum concentration (Tmax) was 0.5 h (range 0.5 to 1.5 hours).
[L50688]
A high-fat meal decreased Cmax by 29% and delayed Tmax to 1.5 hours (range one to three hours), but this difference is not expected to be clinically significant.
[L50688]
Following a cladribine injection given by continuous infusion over seven days, the mean steady-state serum concentration was estimated to be 5.7 ng/mL.
[L50693]
[L50693]
Following oral administration, the terminal half-life is approximately one day.
[L50688]
The intracellular half-life is 15 hours for Cd-AMP and 10 hours for Cd-ATP.
[L50688]
[L50693]
Protein binding is independent of concentration in vitro.
[L50688]
[L50693]
In patients with hematologic malignancies who received a two-hour infusion of cladribine injection at a dose of 0.12 mg/kg, the mean steady-state volume of distribution was 4.5 ± 2.8 L/kg.
[L50693]
Following oral administration, the mean apparent volume of distribution ranges from 480 to 490 L.
[L50688]
Cladribine penetrates into cerebrospinal fluid. One report indicates that concentrations are approximately 25% of those in plasma.
[L50693]
A cerebrospinal fluid:plasma concentration ratio of approximately 0.25 was observed in cancer patients.
[L50688]
The metabolism of cladribine in whole blood has not been fully characterized; however, extensive whole blood and negligible hepatic enzyme metabolism was observed, in vitro.
[L50688]
[L50693]
Following oral administration of 10 mg cladribine in patients with MS, about 28.5% of the dose was excreted unchanged via the renal route. Renal clearance exceeded the glomerular filtration rate, indicating active renal secretion of cladribine.
[L50688]
[L50693]
Proteins and enzymes this drug interacts with in the body
Forms an active ribonucleotide reductase (RNR) complex with RRM1 which is expressed both in resting and proliferating cells in response to DNA damage
These primers are initially extended by the polymerase alpha catalytic subunit and subsequently transferred to polymerase delta and polymerase epsilon for processive synthesis on the lagging and leading strand, respectively. The reason this transfer occurs is because the polymerase alpha has limited processivity and lacks intrinsic 3' exonuclease activity for proofreading error, and therefore is not well suited for replicating long complexes. In the cytosol, responsible for a substantial proportion of the physiological concentration of cytosolic RNA:DNA hybrids, which are necessary to prevent spontaneous activation of type I interferon responses PMID:27019227
Enzymes involved in drug metabolism — important for understanding drug interactions
Proteins that transport this drug across cell membranes
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
PMID:11032837 PMID:15861042 PMID:16446384 PMID:17140564 PMID:21998139
Involved in the homeostasis of endogenous nucleosides .
PMID:11032837 PMID:15861042
Exhibits the transport characteristics of the nucleoside transport system cib or N3 subtype (N3/cib) (with marked transport of both thymidine and inosine) .
PMID:11032837
Employs a 2:1 sodium/nucleoside ratio .
PMID:11032837
Transports uridine .
PMID:21795683
Also able to transport gemcitabine, 3'-azido-3'-deoxythymidine (AZT), ribavirin and 3-deazauridine PMID:11032837 PMID:17140564
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:10722669 PMID:10755314 PMID:12527552 PMID:14759222 PMID:15037197 PMID:17379602 PMID:21795683 PMID:26406980 PMID:27995448 PMID:35790189 PMID:8986748
Functions as a Na(+)-independent transporter .
PMID:8986748
Involved in the transport of nucleosides such as adenosine, guanosine, inosine, uridine, thymidine and cytidine .
PMID:10722669 PMID:10755314 PMID:12527552 PMID:14759222 PMID:15037197 PMID:17379602 PMID:26406980 PMID:8986748
Also transports purine nucleobases (hypoxanthine, adenine, guanine) and pyrimidine nucleobases (thymine, uracil) .
PMID:21795683 PMID:27995448
Mediates basolateral nucleoside uptake into Sertoli cells, thereby regulating the transport of nucleosides in testis across the blood-testis barrier (By similarity). Regulates inosine levels in brown adipocytes tissues (BAT) and extracellular inosine levels, which controls BAT-dependent energy expenditure PMID:35790189
ATC L04AA40
ATC L01BB04
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Cladribine
Additional database identifiers
Drugs Product Database (DPD)
1739
ChemSpider
19105
BindingDB
38920
PDB
CL9
ZINC
ZINC000003798064
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10451
GenAtlas
RRM1
GeneCards
RRM1
GenBank Gene Database
X59543
GenBank Protein Database
36065
Guide to Pharmacology
2630
UniProt Accession
RIR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10452
GenAtlas
RRM2
GeneCards
RRM2
GenBank Gene Database
X59618
Guide to Pharmacology
2631
UniProt Accession
RIR2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:17296
GeneCards
RRM2B
GenBank Gene Database
AB036063
GenBank Protein Database
7229086
UniProt Accession
RIR2B_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9173
GenAtlas
POLA1
GeneCards
POLA1
GenBank Gene Database
X06745
GenBank Protein Database
35568
UniProt Accession
DPOLA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9177
GeneCards
POLE
GenBank Gene Database
L09561
GenBank Protein Database
3192938
UniProt Accession
DPOE1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9178
GeneCards
POLE2
GenBank Gene Database
AF025840
GenBank Protein Database
2697123
UniProt Accession
DPOE2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:13546
GeneCards
POLE3
GenBank Gene Database
AF226077
GenBank Protein Database
8100806
UniProt Accession
DPOE3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:18755
GeneCards
POLE4
GenBank Gene Database
BC031331
GenBank Protein Database
21411517
UniProt Accession
DPOE4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:7892
GenAtlas
NP
GeneCards
PNP
GenBank Gene Database
X00737
GenBank Protein Database
35565
Guide to Pharmacology
2841
UniProt Accession
PNPH_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:186
GenAtlas
ADA
GeneCards
ADA
GenBank Gene Database
X02994
GenBank Protein Database
28380
Guide to Pharmacology
1230
UniProt Accession
ADA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:270
GenAtlas
PARP1
GeneCards
PARP1
GenBank Gene Database
X16674
GenBank Protein Database
1017423
Guide to Pharmacology
2771
UniProt Accession
PARP1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2704
GenAtlas
DCK
GeneCards
DCK
GenBank Gene Database
M60527
UniProt Accession
DCK_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2858
GeneCards
DGUOK
GenBank Gene Database
U41668
GenBank Protein Database
1477482
UniProt Accession
DGUOK_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:74
GenAtlas
ABCG2
GeneCards
ABCG2
GenBank Gene Database
AF103796
GenBank Protein Database
4185796
Guide to Pharmacology
792
UniProt Accession
ABCG2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:16484
GeneCards
SLC28A3
GenBank Gene Database
AF305210
GenBank Protein Database
10732815
Guide to Pharmacology
1116
UniProt Accession
S28A3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11003
GenAtlas
SLC29A1
GeneCards
SLC29A1
GenBank Gene Database
U81375
GenBank Protein Database
1845345
Guide to Pharmacology
1117
UniProt Accession
S29A1_HUMAN
International reference pricing
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
3 active patents, 2 expired
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications: