Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (31)
- 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.
- 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.
- 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 (49)
- 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.
- 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.
- 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)
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%)
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
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.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%
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
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Formulary
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