Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 50mg

Alopecia Areata

Indicated for severe alopecia areata

50 mg PO qDay

Dosage Modifications

Treatment interruption or discontinuation

  • Temporary treatment interruption for <6 weeks is not expected to result in significant loss of regrown scalp hair

Hematologic abnormalities

  • Platelet count <50,000/mm3: Discontinue treatment
  • Absolute lymphocyte count (ALC) <500/mm3: Interrupt treatment; may restart once ALC returns above this value

Renal impairment

  • Mild-to-moderate (eGFR 30-89 mL/min): Not studied as a clinically relevant increase in exposure is not expected
  • Severe (eGFR <30 mL/min): AUC24 was 55.2% higher compared with participants with normal renal functions; these differences were not considered clinically significant
  • ESRD or in renal transplant recipients: Not studied

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): No dosage adjustment required
  • Severe (Child-Pugh C): Not recommended

Dosing Considerations

Limitations of use

  • Not recommended for use in combination with other JAK inhibitors, biologic immunomodulators, cyclosporine, or other potent immunosuppressants

Before initiating

  • Evaluation for tuberculosis (TB) infection; do not initiate with active TB
  • For patients with latent TB or those with a negative latent TB test who are at high risk for TB, start preventive therapy for latent TB before initiating
  • Screen for viral hepatitis in accordance with clinical guidelines; do not initiate in patients with hepatitis B or hepatitis C
  • Do not initiate if ALC <500/mm3 or platelet count <100,000/mm3
  • Update immunizations according to current immunization guidelines

Monitoring

  • ALC and platelet counts recommended at 4 weeks after treatment initiation, and thereafter according to routine patient management

Dosage Forms & Strengths

capsule

  • 50mg

Alopecia Areata

Indicated for severe alopecia areata in patients aged ≥12 years

<12 years: Safety and efficacy not established

≥12 years: 50 mg PO qDay

Dosage Modifications

Treatment interruption or discontinuation

  • Temporary treatment interruption for <6 weeks is not expected to result in significant loss of regrown scalp hair

Hematologic abnormalities

  • Platelet count <50,000/mm3: Discontinue treatment
  • Absolute lymphocyte count (ALC) <500/mm3: Interrupt treatment; may restart once ALC returns above this value

Renal impairment

  • Mild-to-moderate (eGFR 30-89 mL/min): Not studied as a clinically relevant increase in exposure is not expected
  • Severe (eGFR <30 mL/min): AUC24 was 55.2% higher compared with participants with normal renal functions; these differences were not considered clinically significant
  • ESRD or in renal transplant recipients: Not studied

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): No dosage adjustment required
  • Severe (Child-Pugh C): Not recommended

Dosing Considerations

Limitations of use

  • Not recommended for use in combination with other JAK inhibitors, biologic immunomodulators, cyclosporine, or other potent immunosuppressants

Before initiating

  • Evaluation for tuberculosis (TB) infection; do not initiate with active TB
  • For patients with latent TB or those with a negative latent TB test who are at high risk for TB, start preventive therapy for latent TB before initiating
  • Screen for viral hepatitis in accordance with clinical guidelines; do not initiate in patients with hepatitis B or hepatitis C
  • Do not initiate if ALC <500/mm3 or platelet count <100,000/mm3
  • Update immunizations according to current immunization guidelines

Monitoring

  • ALC and platelet counts recommended at 4 weeks after treatment initiation, and thereafter according to routine patient management
Next:

Interactions

Interaction Checker

and ritlecitinib

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (33)

              • adenovirus types 4 and 7 live, oral

                ritlecitinib, adenovirus types 4 and 7 live, oral. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • apalutamide

                apalutamide will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • BCG vaccine live

                ritlecitinib, BCG vaccine live. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • carbamazepine

                carbamazepine will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • cholera vaccine

                ritlecitinib, cholera vaccine. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • dengue vaccine

                ritlecitinib, dengue vaccine. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • Ebola Zaire vaccine

                ritlecitinib, Ebola Zaire vaccine. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • enzalutamide

                enzalutamide will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • fosphenytoin

                fosphenytoin will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • influenza virus vaccine quadrivalent, intranasal

                ritlecitinib, influenza virus vaccine quadrivalent, intranasal. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • lumacaftor/ivacaftor

                lumacaftor/ivacaftor will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • measles (rubeola) vaccine

                ritlecitinib, measles (rubeola) vaccine. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • measles mumps and rubella vaccine, live

                ritlecitinib, measles mumps and rubella vaccine, live. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • measles, mumps, rubella and varicella vaccine, live

                ritlecitinib, measles, mumps, rubella and varicella vaccine, live. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • mitotane

                mitotane will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • nirogacestat

                ritlecitinib will increase the level or effect of nirogacestat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • phenobarbital

                phenobarbital will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • phenytoin

                phenytoin will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • poliovirus vaccine live oral trivalent

                ritlecitinib, poliovirus vaccine live oral trivalent. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • primidone

                primidone will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • repotrectinib

                ritlecitinib will increase the level or effect of repotrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Discontinue strong or moderate CYP3A inhibitors and wait 3-5 elimination half-lives before initiating repotrectinib.

              • rifampin

                rifampin will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • rotavirus oral vaccine, live

                ritlecitinib, rotavirus oral vaccine, live. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • rubella vaccine

                ritlecitinib, rubella vaccine. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • smallpox (vaccinia) and monkeypox vaccine, live, nonreplicating

                ritlecitinib, smallpox (vaccinia) vaccine, attenuated. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • smallpox (vaccinia) vaccine, attenuated

                ritlecitinib, smallpox (vaccinia) vaccine, attenuated. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • smallpox (vaccinia) vaccine, live

                ritlecitinib, smallpox (vaccinia) vaccine, live. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • St John's Wort

                St John's Wort will decrease the level or effect of ritlecitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy.

              • typhoid polysaccharide vaccine

                ritlecitinib, typhoid polysaccharide vaccine. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • typhoid vaccine live

                ritlecitinib, typhoid vaccine live. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • varicella virus vaccine live

                ritlecitinib, varicella virus vaccine live. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • yellow fever vaccine

                ritlecitinib, yellow fever vaccine. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              • zoster vaccine live

                ritlecitinib, zoster vaccine live. immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid live attenuated vaccines during or shortly before initiating ritlecitinib. No data are available on vaccination response in ritlecitinib treated patients. Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines.

              Monitor Closely (51)

              • alfentanil

                ritlecitinib will increase the level or effect of alfentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • alosetron

                ritlecitinib will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • bendamustine

                ritlecitinib will increase the level or effect of bendamustine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • capivasertib

                ritlecitinib will increase the level or effect of capivasertib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce capivasertib dose if coadministered with moderate CYP3A inhibitors.

              • carbamazepine

                ritlecitinib will increase the level or effect of carbamazepine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • clomipramine

                ritlecitinib will increase the level or effect of clomipramine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • clonidine

                ritlecitinib will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • clozapine

                ritlecitinib will increase the level or effect of clozapine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • colchicine

                ritlecitinib will increase the level or effect of colchicine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • cyclosporine

                ritlecitinib will increase the level or effect of cyclosporine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • dihydroergotamine

                ritlecitinib will increase the level or effect of dihydroergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • disopyramide

                ritlecitinib will increase the level or effect of disopyramide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • divalproex sodium

                ritlecitinib will increase the level or effect of divalproex sodium by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • duloxetine

                ritlecitinib will increase the level or effect of duloxetine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • ergotamine

                ritlecitinib will increase the level or effect of ergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • ethosuximide

                ritlecitinib will increase the level or effect of ethosuximide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • everolimus

                ritlecitinib will increase the level or effect of everolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • fentanyl

                ritlecitinib will increase the level or effect of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • fluvoxamine

                ritlecitinib will increase the level or effect of fluvoxamine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • fosphenytoin

                ritlecitinib will increase the level or effect of fosphenytoin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • gepirone

                ritlecitinib will increase the level or effect of gepirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce gepirone dose by 50% when used concomitantly with a moderate CYP3A4 inhibitor.

              • melatonin

                ritlecitinib will increase the level or effect of melatonin by additive vasodilation. Use Caution/Monitor. Monitor melatonin effects if coadministered with moderate CYP1A2 inhibitors

              • mexiletine

                ritlecitinib will increase the level or effect of mexiletine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • midazolam

                ritlecitinib will increase the level or effect of midazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • norgestrel

                ritlecitinib will increase the level or effect of norgestrel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Strong or moderate CYP3A4 inhibitors may increase systemic concentration of norgestrel, which may increase risk for adverse effects

              • olanzapine

                ritlecitinib will increase the level or effect of olanzapine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • pacritinib

                ritlecitinib will increase the level or effect of pacritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • palovarotene

                ritlecitinib will increase the level or effect of palovarotene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of palovarotene, a CYP3A substrate, with moderate CYP3A inhibitors. If unavoidable, reduce palovarotene dose by 50%.

              • phenobarbital

                ritlecitinib will increase the level or effect of phenobarbital by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • phenytoin

                ritlecitinib will increase the level or effect of phenytoin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • pimozide

                ritlecitinib will increase the level or effect of pimozide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • pirfenidone

                ritlecitinib will increase the level or effect of pirfenidone by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • pomalidomide

                ritlecitinib will increase the level or effect of pomalidomide by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • primidone

                ritlecitinib will increase the level or effect of primidone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • quinidine

                ritlecitinib will increase the level or effect of quinidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • quinine

                ritlecitinib will increase the level or effect of quinine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • ramelteon

                ritlecitinib will increase the level or effect of ramelteon by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • rasagiline

                ritlecitinib will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • repaglinide

                ritlecitinib will increase the level or effect of repaglinide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • riluzole

                ritlecitinib will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • ropinirole

                ritlecitinib will increase the level or effect of ropinirole by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • sirolimus

                ritlecitinib will increase the level or effect of sirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • tacrolimus

                ritlecitinib will increase the level or effect of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • tasimelteon

                ritlecitinib will increase the level or effect of tasimelteon by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • theophylline

                ritlecitinib will increase the level or effect of theophylline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

                ritlecitinib will increase the level or effect of theophylline by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • thioridazine

                ritlecitinib will increase the level or effect of thioridazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • tizanidine

                ritlecitinib will increase the level or effect of tizanidine by affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP1A2 substrates.

              • triazolam

                ritlecitinib will increase the level or effect of triazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • ublituximab

                ublituximab and ritlecitinib both increase immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Owing to potential additive immunosuppressive effects, consider duration of effect and mechanism of action of these therapies if coadministered

              • valproic acid

                ritlecitinib will increase the level or effect of valproic acid by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              • warfarin

                ritlecitinib will increase the level or effect of warfarin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Ritlecitinib inhibits CYP3A4 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions. Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A substrates.

              Minor (0)

                Previous
                Next:

                Adverse Effects

                >10%

                Headache (10.8%)

                1-10%

                Diarrhea (10%)

                Acne (6.2%)

                Rash (5.4%)

                Urticaria (4.6%)

                Folliculitis (3.1%)

                Pyrexia (3.1%)

                Atopic dermatitis (2.3%)

                Dizziness (2.3%)

                Increased CPK (1.5%)

                Herpes zoster (1.5%)

                Decreased RBCs (1.5%)

                Stomatitis (1.5%)

                Previous
                Next:

                Warnings

                Black Box Warnings

                Serious infections

                • Increased risk of serious bacterial, fungal, viral and opportunistic infections leading to hospitalization or death, including tuberculosis (TB)
                • Interrupt treatment if serious infection occurs until the infection is controlled
                • Do not prescribe to patients with active TB; test for latent TB before and during therapy; treat latent TB prior to use
                • Monitor all patients for active TB during treatment, even patients with initial negative, latent TB test

                Increased mortality

                • Higher rate of all-cause mortality, including sudden cardiovascular (CV) death with another Janus kinase inhibitor (JAK) compared with TNF blockers in patients with rheumatoid arthritis (RA)
                • Ritlecitinib is not approved for use in RA

                Malignancies

                • Malignancies have occurred
                • Higher rate of lymphomas and lung cancers with another JAK inhibitor compared with TNF blockers patients with RA

                MACE

                • Higher rate of major adverse cardiovascular events (MACE), defined as CV death, myocardial infarction, and stroke, with another JAK inhibitor compared with TNF blockers in patients with RA

                Thrombosis

                • Thrombosis has occurred
                • Increased incidence of pulmonary embolism, venous and arterial thrombosis with another JAK inhibitor compared with TNF blockers

                Contraindications

                Known hypersensitivity to ritlecitinib or any of its excipients

                Cautions

                In a large, randomized, postmarketing safety study of another JAK inhibitor in patients with RA aged ≥50 years with at least 1 CV risk factor, a higher rate of all-cause mortality, including sudden CV death, was observed in patients treated with the JAK inhibitor compared TNF blockers

                Similarly, increased risk for MACE and thromboembolic events were observed with another JAK inhibitor in patients with RA aged ≥50 years; avoid in patients who may be at increased risk of thrombosis; if symptoms of thrombosis or embolism occur, patients should interrupt therapy and be evaluated promptly and treated appropriately

                Malignancies, including non-melanoma skin cancer (NMSC), were observed in clinical trial; consider risks and benefits of treatment before initiating or continuing therapy in patients with known malignancy other than a successfully treated NMSC or cervical cancer; perform periodic skin examination for patients who are at increased risk for skin cancer

                Consider benefits and risks for individual patient prior to initiating or continuing therapy with, particularly in patients who are current or past smokers and patients with other cardiovascular risk factors; patients should be informed about symptoms of serious cardiovascular events and steps to take if they occur; discontinue in patients that have experienced myocardial infarction or stroke

                Serious reactions including anaphylactic reactions, urticaria and rash observed in clinical trials; discontinue and institute appropriate therapy if clinically significant rash occurs

                Serious infections

                • Serious infections reported; common serious infections reported were appendicitis, COVID-19 infection (including pneumonia), and sepsis; among opportunistic infections, multidermatomal herpes zoster was reported
                • Avoid use with an active, serious infection
                • Consider the risks and benefits of treatment before initiating in patients
                  • With chronic or recurrent infection
                  • Who have been exposed to TB
                  • With history of serious infection or an opportunistic infection
                  • Who have resided or traveled in areas of endemic TB or mycoses, or
                  • With underlying conditions that may predispose them to infection
                • Screen for TB and viral hepatitis before initiating
                • Monitor for viral reactivation, including herpes zoster
                • Caution in patients with HIV or other immunocompromised conditions
                • Patients who develops new infections during treatment should undergo prompt and complete diagnostic testing appropriate for an immunocompromised patient; initiate appropriate antimicrobial and closely monitor; therapy may be resumed once infection controlled
                • If patient develops herpes zoster, consider interrupting treatment until episode resolves

                Laboratory abnormalities

                • Treatment associated with decreased lymphocytes and platelets
                • Evaluate ALC, platelet counts, and liver enzymes at baseline and thereafter according to routine patient management
                • Elevated CPK observed compared with placebo

                Drug interaction overview

                • Inhibitor of CYP3A4 and CYP1A2
                • Substrate of CYP3A
                • Vaccinations
                  • Avoid live attenuated vaccines during or shortly before initiating treatment
                  • No data are available on vaccination response in ritlecitinib treated patients
                  • Before initiating, review patient immunization status (including herpes zoster) and immunize accordingly in agreement with current immunization guidelines
                • Strong CYP3A4 inducers
                  • Avoid
                  • Coadministration with strong CYP3A inducers may decrease ritlecitinib AUC and peak plasma concentration, which may result in loss of or reduced efficacy
                • Sensitive CYP3A4 or CYP1A2 substrates
                  • Monitor/modify dose of sensitive CYP3A4/CYP1A2 substrates
                  • Ritlecitinib inhibits CYP3A4 and CYP1A2 substrates; coadministration increases AUC and peak plasma concentration sensitive substrates, which may increase risk of adverse reactions
                  • Additional monitoring and dosage adjustment may be needed in accordance with product labeling of CYP3A or CYP1A2 substrates
                Previous
                Next:

                Pregnancy & Lactation

                Pregnancy

                Data from clinical trials are insufficient regarding use in pregnant females to identify drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes

                Pregnancy registry: Report exposures during pregnancy by calling 1-877-390-2940

                Animal studies

                • Oral administration to pregnant rats and rabbits during organogenesis caused fetotoxicity and fetal malformations at exposures 49 and 55 times the maximum recommended human dose (MRHD) based on AUC comparison, respectively

                Lactation

                Data are unavailable on presence  in human milk, effects on breastfed infants, or effects on milk production

                Ritlecitinib is present in milk of lactating rats; when a drug is present in animal milk, it is likely that it will be present in human milk

                Owing to the serious adverse effects in adults, including risks of serious infection and malignancy, advise females not to breastfeed during treatment and for ~14 hr after last dose (~6 elimination half-lives)

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

                Previous
                Next:

                Pharmacology

                Mechanism of Action

                Irreversibly inhibits Janus kinase 3 (JAK3) and the tyrosine kinase expressed in hepatocellular carcinoma (TEC) kinase family by blocking adenosine triphosphate (ATP) binding site

                In cellular settings, ritlecitinib inhibits cytokine induced STAT phosphorylation mediated by JAK3-dependent receptors

                Additionally, ritlecitinib inhibits signaling of immune receptors dependent on TEC kinase family members; relevance of inhibition of specific JAK or TEC family enzymes to therapeutic effectiveness is not currently known

                Absorption

                Bioavailability ~64%

                Peak plasma time: 1 hr

                Steady-state reach ~4 days

                Food

                • Food does not have a clinically significant impact on systemic exposure
                • High-fat meal reduced peak plasma concentration by ~32% and AUCinf was increased by 11%

                Distribution

                Protein bound: ~14%

                Metabolism

                Metabolism is mediated by multiple pathways with no single route contributing >25% of total metabolism

                Metabolic pathways include

                • Glutathione S-transferase (GST): cytosolic GST A1/3, M1/3/5, P1, S1, T2, Z1 and microsomal GST 1/2/3
                • CYP enzymes (CYP3A, CYP2C8, CYP1A2, and CYP2C9)

                Elimination

                Half-life: 1.3-2.3 hr

                Excretion: Urine 66% (~4% unchanged); feces 20%

                Previous
                Next:

                Administration

                Oral Administration

                May take with or without food

                Swallow capsule whole; do not crush, split, or chew

                Missed dose

                • Administer missed dose as soon as possible unless it is <8 hr before next dose, then skip the missed dose
                • Thereafter, resume dosing regular scheduled time

                Storage

                Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

                Keep in original package

                Previous
                Next:

                Images

                No images available for this drug.
                Previous
                Next:

                Patient Handout

                A Patient Handout is not currently available for this monograph.
                Previous
                Next:

                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

                To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                Adding plans allows you to:

                • View the formulary and any restrictions for each plan.
                • Manage and view all your plans together – even plans in different states.
                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
                Additional Offers
                Email to Patient

                From:

                To:

                The recipient will receive more details and instructions to access this offer.

                By clicking send, you acknowledge that you have permission to email the recipient with this information.

                Email Forms to Patient

                From:

                To:

                The recipient will receive more details and instructions to access this offer.

                By clicking send, you acknowledge that you have permission to email the recipient with this information.

                Previous
                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.