Purine Antimetabolite

Cladribine

Approved 27 Mar 2026OralTablet

The FDA lists this product in 6 strengths and forms.

Indications

Cladribine is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include relapsing-remitting disease and active secondary progressive disease, in adults. Because of its safety profile, 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 [see Warnings and Precautions (5) ].

Cladribine is a purine antimetabolite indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include relapsing-remitting disease and active secondary progressive disease, in adults. Because of its safety profile, 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. ( 1 , 5 ) Limitations of Use Cladribine is not recommended for use in patients with clinically isolated syndrome (CIS) because of its safety profile .

( 1 , 5 ) Limitations of Use Cladribine is not recommended for use in patients with clinically isolated syndrome (CIS) because of its safety profile [see Warnings and Precautions (5) ].

Contraindications

Cladribine is contraindicated: in patients with current malignancy [see Warnings and Precautions (5.1) ]. in pregnant women and in women and men of reproductive potential who do not plan to use effective contraception during cladribine dosing and for 6 months after the last dose in each treatment course. May cause fetal harm [see Warnings and Precautions (5.2) and Use in Specific Populations (8.1 , 8.3) ] . in patients infected with the human immunodeficiency virus (HIV ) [see Warnings and Precautions (5.4) ]. in patients with active chronic infections (e.g., hepatitis or tuberculosis) [see Warnings and Precautions (5.4) ]. in patients with a history of hypersensitivity to cladribine [see Warnings and Precautions (5.8) ]. in women intending to breastfeed on a cladribine treatment day and for 10 days after the last dose [see Use in Specific Populations (8.2) ].

Patients with current malignancy. ( 4 ) Pregnant women, and women and men of reproductive potential who do not plan to use effective contraception during cladribine dosing and for 6 months after the last dose in each treatment course. ( 4 , 8.3 ) HIV infection. ( 4 ) Active chronic infections (e.g., hepatitis or tuberculosis). ( 4 ) History of hypersensitivity to cladribine. ( 4 , 5.8 ) Women intending to breastfeed on a cladribine treatment day and for 10 days after the last dose.

( 4 , 8.2 )

At a glance

Brand name: Cladribine
Pharmacologic class: Purine Antimetabolite
Route: Oral
Dosage form: Tablet
Applicant: Hopewell Pharma
Status: Prescription
FDA approval: 27 Mar 2026
Application: ANDA215547-001

Indications

( 1 , 5 ) Limitations of Use Cladribine is not recommended for use in patients with clinically isolated syndrome (CIS) because of its safety profile [see Warnings and Precautions (5) ].

Contraindications

( 4 , 8.2 )

Interactions

Table 3 Drug Interactions with Cladribine

7.1Immunomodulatory, Immunosuppressive, or Myelosuppressive Drugs Clinical Impact

Concomitant use of cladribine with immunomodulatory, immunosuppressive, or myelosuppressive drugs may increase the risk of adverse reactions because of the additive effects on the immune system [see Warnings and Precautions (5.4) ] . Prevention or Management Concomitant use with myelosuppressive or other immunosuppressive drugs is not recommended. Acute short- term therapy with corticosteroids can be administered. In patients who have previously been treated with immunomodulatory or immunosuppressive drugs, consider potential additive effect, the mode of action, and duration of effect of the other drugs prior to initiation of cladribine.

7.2Interferon-Beta Clinical Impact

Concomitant use of cladribine with interferon-beta did not change the exposure of cladribine to a clinically significant effect; however, lymphopenia risk may be increased [see Warnings and Precautions (5.3) ]. Prevention or Management Concomitant use is not recommended.

7.3Hematotoxic Drugs Clinical Impact

Concomitant use of cladribine with hematotoxic drugs may increase the risk of adverse reactions because of the additive hematological effects [see Warnings and Precautions (5.5) ]. Prevention or Management Monitor hematological parameters.

7.4Antiviral and Antiretroviral Drugs Clinical Impact

Compounds that require intracellular phosphorylation to become active (e.g., lamivudine, zalcitabine, ribavirin, stavudine, and zidovudine) could interfere with the intracellular phosphorylation and activity of cladribine. Prevention or Management Avoid concomitant use .

7.5Potent ENT, CNT and BCRP Transporter Inhibitors Clinical Impact

Cladribine is a substrate of breast cancer resistance protein (BCRP), equilibrative nucleoside (ENT1), and concentrative nucleoside (CNT3) transport proteins. The bioavailability, intracellular distribution, and renal elimination of cladribine may be altered by potent ENT1, CNT3, and BCRP transporter inhibitors. Prevention or Management Avoid co-administration of potent ENT1, CNT3, or BCRP transporter inhibitors (e.g., ritonavir, eltrombopag, curcumin, cyclosporine, dilazep, nifedipine, nimodipine, cilostazol, sulindac, dipyridamole, or reserpine) during the 4 to 5 day cladribine treatment cycles.

If this is not possible, consider selection of alternative concomitant drugs with no or minimal ENT1, CNT3, or BCRP transporter inhibiting properties. If this is not possible, dose reduction to the minimum mandatory dose of drugs containing these compounds, separation in the timing of administration, and careful patient monitoring is recommended.

7.6Potent BCRP and P-gp Transporter Inducers Clinical Impact

Possible decrease in cladribine exposure if potent BCRP or P-gp transporter inducers are co-administered. Prevention or Management Consider a possible decrease in cladribine efficacy if potent BCRP (e.g., corticosteroids) or P-gp (e.g., rifampicin, St. John's Wort) transporter inducers are co-administered. Immunosuppressive drugs: Consider overlapping effects on immune system, when used sequentially. Concomitant use not recommended.

( 7.1 ) Hematotoxic drugs: Monitor patients for additive effects on the hematological profile. ( 7.3 ) Antiviral and antiretroviral drugs: Avoid concomitant use. ( 7.4 ) BCRP or ENT/CNT inhibitors: May alter bioavailability of cladribine. Avoid concomitant use. ( 7.5 )

Adverse reactions

The following serious adverse reactions and potential risks are discussed, or discussed in greater detail, in other sections of the labeling: Malignancies [see Warnings and Precautions (5.1) ] Risk of Teratogenicity [see Warnings and Precautions (5.2) ] Lymphopenia [see Warnings and Precautions (5.3) ] Infections [see Warnings and Precautions (5.4) ] Hematologic Toxicity [see Warnings and Precautions (5.5) ] Graft-Versus-Host Disease With Blood Transfusion [see Warnings and Precautions (5.6) ] Liver Injury [see Warnings and Precautions (5.7) ] Hypersensitivity [see Warnings and Precautions (5.8) ] Cardiac Failure [see Warnings and Precautions (5.9) ] Most common adverse reactions (incidence > 20%) are upper respiratory tract infection, headache, and lymphopenia.

( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hopewell at 1-888-922-2116, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

6.1Clinical Trials Experience

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. In the clinical trial program of cladribine in MS, 1,976 patients received cladribine for a total of 9,509 patient years. The mean time on study including follow-up was approximately 4.8 years, and approximately 24% of cladribine-treated patients had approximately 8 years of time on study including follow-up.

Of these, 923 patients aged 18 to 66 years received cladribine as monotherapy at a cumulative dose of 3.5 mg per kg. Table 2 shows adverse reactions in Study 1 [see Clinical Studies (14) ] with an incidence of at least 5% for cladribine and higher than placebo. The most common (> 20%) adverse reactions reported in Study 1 are upper respiratory tract infection, headache, and lymphopenia. Table 2 Adverse Reactions in Study 1 with an Incidence of at Least 5% for Cladribine and Higher than Placebo Cladribine (N=440) % Placebo (N=435) % Upper respiratory tract infection 38 32 Headache 25 19 Lymphopenia 24 2 Nausea 10 9 Back pain 8 6 Arthralgia and arthritis 7 5 Insomnia 6 4 Bronchitis 5 3 Hypertension 5 3 Fever 5 3 Depression 5 3 Hypersensitivity In clinical studies, 11% of cladribine patients had hypersensitivity adverse reactions, compared to 7% of placebo patients [see Warnings and Precautions (5.8) ].

Alopecia Alopecia occurred in 3% of cladribine-treated patients compared to 1% of placebo patients. Myelodysplastic Syndrome Cases of myelodysplastic syndrome have been reported in patients that had received parenteral cladribine at a higher dosage than that approved for cladribine. These cases occurred several years after treatment. Herpes Meningoencephalitis Fatal herpes meningoencephalitis occurred in one cladribine-treated patient, at a higher dosage and longer duration of therapy than the approved cladribine dosage and in combination with interferon beta-1a treatment.

Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) SJS and TEN are identified risks of parenteral cladribine for the treatment of oncologic indications. Seizures In clinical studies, serious events of seizure occurred in 0.3% of cladribine-treated patients compared to 0 placebo patients. Serious events included generalized tonic-clonic seizures and status epilepticus. It is unknown whether these events were related to the effects of multiple sclerosis alone, to cladribine, or to a combination of both.

6.2Postmarketing Experience

The following adverse reactions have been identified during postapproval use of cladribine. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Infections and Infestations: nocardiosis, varicella zoster, histoplasmosis, cryptococcosis, and toxoplasmosis [see Warnings and Precautions (5.4) ] Hepatobiliary Disorders: liver injury [see Warnings and Precautions (5.7) ]

Cladribine

Indications

Contraindications

At a glance

Two medicines in one question?

Cladribine

Indications

Contraindications

At a glance

Two medicines in one question?

Warnings and precautions

5.1Malignancies Treatment

5.2Risk of Teratogenicity

5.3Lymphopenia

5.4Infections

Interactions

7.1Immunomodulatory, Immunosuppressive, or Myelosuppressive Drugs Clinical Impact

7.2Interferon-Beta Clinical Impact

7.3Hematotoxic Drugs Clinical Impact

7.4Antiviral and Antiretroviral Drugs Clinical Impact

7.5Potent ENT, CNT and BCRP Transporter Inhibitors Clinical Impact

7.6Potent BCRP and P-gp Transporter Inducers Clinical Impact

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary

Adverse reactions

6.1Clinical Trials Experience

6.2Postmarketing Experience

Composition

Strengths and forms

Official product information