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Velsipity
etrasimod
Adult Dosing .
Dosage forms: TAB: 2 mg
ulcerative colitis, moderate-severe
- [2 mg PO qd]
renal dosing
- [not defined]
- renal impairment: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class C: avoid use
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- pregnancy
- hepatic impairment, Child-Pugh Class C
- infection, active
- MI w/in 6mo
- unstable angina w/in 6mo
- stroke w/in 6mo
- TIA w/in 6mo
- decompensated heart failure w/ hospitalization w/in 6mo
- NYHA Class III-IV CHF w/in 6mo
- AV block, 2nd-3rd degree (pts w/o pacemaker)
- AV block hx, 2nd-3rd degree (pts w/o pacemaker)
- sick sinus syndrome (pts w/o pacemaker)
- sick sinus syndrome hx (pts w/o pacemaker)
- sino-atrial block (pts w/o pacemaker)
- sino-atrial block hx (pts w/o pacemaker)
- phototherapy, concurrent
- avoid: sun exposure
- avoid: UV light exposure, artificial
- caution: pts of childbearing potential
- caution: electrolyte abnormalities
- caution: AV block risk
- caution: bradycardia risk
- caution: QTc >470 msec (female pts)
- caution: QTc >450 msec (male pts)
- caution: long QT syndrome, congenital
- caution: QT prolongation family hx
- caution: torsades de pointes hx
- caution: ventricular arrhythmia
- caution: sleep apnea, severe untreated
- caution: infection risk
Drug Interactions .
Overview
etrasimod
S1P modulator
- CYP2C8 substrate
- CYP2C9 substrate
- CYP3A4 substrate
- bradycardia
- delays atrioventricular conduction
- hypertensive effects
- immunosuppressive effects
- prolongs QT interval (conditional)
Contraindicated
- adenovirus vaccine, live
- BCG live intravesical
- chikungunya vaccine, live
- cholera vaccine, live
- dengue vaccine, live
- influenza nasal vaccine, live
- measles/mumps/rubella vaccine, live
- pimozide
- rotavirus vaccine, live
- smallpox vaccine, live
- talimogene laherparepvec
- thioridazine
- typhoid vaccine, live
- varicella vaccine, live
- yellow fever vaccine, live
Avoid/Use Alternative
- abatacept
- abemaciclib
- abrocitinib
- acalabrutinib
- acebutolol
- adagrasib
- adalimumab
- adenosine
- afamitresgene autoleucel
- aldesleukin
- alectinib
- alemtuzumab
- alfentanil
- amiodarone
- anagrelide
- anakinra
- anifrolumab
- anti-thymocyte globulin
- apalutamide
- apomorphine
- apraclonidine ophthalmic
- aprepitant
- arsenic trioxide
- artemether/lumefantrine
- articaine
- asciminib
- asenapine
- atazanavir
- atenolol
- atidarsagene autotemcel
- avacopan
- axicabtagene ciloleucel
- azacitidine
- azathioprine
- azithromycin
- baricitinib
- basiliximab
- bedaquiline
- belatacept
- belimumab
- belinostat
- bendamustine
- berotralstat
- betaxolol
- betaxolol ophthalmic
- bimekizumab
- bisoprolol
- blinatumomab
- bortezomib
- brentuximab vedotin
- brexucabtagene autoleucel
- brigatinib
- brodalumab
- bupivacaine
- bupivacaine liposomal
- busulfan
- cabazitaxel
- cabozantinib
- canakinumab
- carbamazepine
- carboplatin
- carfilzomib
- carmustine
- carteolol ophthalmic
- carvedilol
- ceritinib
- certolizumab pegol
- chlorambucil
- chloramphenicol
- chloroprocaine
- chloroquine
- ciltacabtagene autoleucel
- cimetidine
- ciprofloxacin
- cisapride
- cisplatin
- citalopram
- cladribine injection
- cladribine oral
- clarithromycin
- clobetasol ophthalmic
- clofarabine
- clofazimine
- clonidine
- clopidogrel
- clozapine
- cobicistat
- conivaptan
- copanlisib
- corticotropin
- crizotinib
- crovalimab
- cyclophosphamide
- cyclosporine
- cytarabine
- dactinomycin
- danazol
- danicopan
- daratumumab
- darunavir
- daunorubicin
- decitabine
- deferasirox
- degarelix
- desflurane
- desipramine
- deucravacitinib
- deuruxolitinib
- dexmedetomidine
- dexmedetomidine injection
- digoxin
- diltiazem
- dimethyl fumarate
- dinutuximab
- diroximel fumarate
- disopyramide
- docetaxel
- dofetilide
- domperidone
- donepezil
- doxorubicin
- dronedarone
- droperidol
- dulaglutide
- dupilumab
- duvelisib
- eculizumab
- efavirenz
- efgartigimod alfa
- eliglustat
- elivaldogene autotemcel
- elotuzumab
- elranatamab
- emapalumab
- encorafenib
- ensartinib
- epcoritamab
- ephedra
- epinephrine inhaled
- epirubicin
- eribulin
- erythromycin
- esmolol
- etanercept
- etoposide
- everolimus
- famotidine
- fedratinib
- fentanyl
- fexinidazole
- fingolimod
- flecainide
- floxuridine
- fluconazole
- fludarabine
- fluorouracil
- fosamprenavir
- fosphenytoin
- fruquintinib
- furosemide
- galantamine
- gemcitabine
- gemfibrozil
- gemtuzumab ozogamicin
- gilteritinib
- glasdegib
- glofitamab
- golimumab
- goserelin
- grapefruit
- guanfacine
- guselkumab
- haloperidol
- histrelin
- hydroxychloroquine
- hydroxyurea
- hydroxyzine
- ibritumomab tiuxetan
- ibrutinib
- ibutilide
- idarubicin
- idecabtagene vicleucel
- idelalisib
- ifosfamide
- imatinib
- inebilizumab
- infliximab
- inotuzumab ozogamicin
- iptacopan
- irinotecan
- isatuximab
- isavuconazonium
- isoflurane
- itraconazole
- ivabradine
- ivosidenib
- ixabepilone
- ixekizumab
- ketoconazole
- labetalol
- lacosamide
- lamotrigine
- landiolol
- lanreotide
- lasmiditan
- lebrikizumab
- lefamulin
- leflunomide
- lenacapavir
- lenalidomide
- letermovir
- leuprolide
- levobunolol ophthalmic
- levofloxacin
- levoketoconazole
- lidocaine
- lisocabtagene maraleucel
- lithium
- lofexidine
- lomustine
- lonafarnib
- loncastuximab tesirine
- lopinavir/ritonavir
- lorlatinib
- lymphocyte immune globulin, anti-thymocyte globulin
- macimorelin
- mefloquine
- melphalan
- mepivacaine
- mercaptopurine
- methadone
- methotrexate
- metoprolol
- midodrine
- mifepristone
- milk thistle
- mirikizumab
- mitoxantrone
- mobocertinib
- mogamulizumab
- momelotinib
- monomethyl fumarate
- mosunetuzumab
- moxifloxacin
- mycophenolate mofetil
- mycophenolic acid
- nadolol
- natalizumab
- nebivolol
- nefazodone
- nelarabine
- nelfinavir
- neostigmine
- netupitant
- nilotinib
- nirogacestat
- nitisinone
- obecabtagene autoleucel
- obinutuzumab
- ocrelizumab
- octreotide
- ofatumumab
- oliceridine
- ondansetron
- osimertinib
- oxaliplatin
- ozanimod
- paclitaxel
- pacritinib
- paliperidone
- palonosetron
- panobinostat
- pasireotide
- pegcetacoplan
- pentamidine
- pentostatin
- phenytoin
- pimecrolimus topical
- pindolol
- pirtobrutinib
- polatuzumab vedotin
- pomalidomide
- ponatinib
- ponesimod
- posaconazole
- pozelimab
- praziquantel
- procainamide
- procarbazine
- propafenone
- propranolol
- pyridostigmine
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- quizartinib
- rabies vaccine
- ravulizumab
- regadenoson
- regorafenib
- remifentanil
- remimazolam
- revumenib
- ribociclib
- rifampin
- rilonacept
- risankizumab
- ritlecitinib
- ritonavir
- rituximab
- rivastigmine
- romidepsin
- ropeginterferon alfa-2b
- ropivacaine
- rozanolixizumab
- rucaparib
- ruxolitinib
- ruxolitinib topical
- sarilumab
- satralizumab
- secukinumab
- selinexor
- selpercatinib
- sevoflurane
- siltuximab
- siponimod
- sirolimus
- sirolimus albumin-bound
- sotalol
- spesolimab
- succinylcholine
- sufentanil
- sugammadex
- sulfasalazine
- sutimlimab
- tacrolimus
- tafasitamab
- talquetamab
- tarlatamab
- teclistamab
- telavancin
- temozolomide
- temsirolimus
- teplizumab
- teriflunomide
- tetrabenazine
- thalidomide
- thioguanine
- thiotepa
- ticagrelor
- tildrakizumab
- timolol
- timolol ophthalmic
- tipranavir
- tisagenlecleucel
- tocilizumab
- tofacitinib
- topotecan
- toremifene
- tralokinumab
- tramadol
- triclabendazole
- trifluridine
- triptorelin
- tucatinib
- ublituximab
- upadacitinib
- ustekinumab
- vandetanib
- vedolizumab
- vemurafenib
- venetoclax
- verapamil
- vilobelimab
- vinblastine
- vincristine
- vinorelbine
- voclosporin
- voriconazole
- zanubrutinib
- zilucoplan
- ziprasidone
Monitor/Modify Tx
- abiraterone acetate
- albuterol
- albuterol inhaled
- aliskiren
- almotriptan
- amiloride
- amitriptyline
- amlodipine
- amoxapine
- amphetamine
- angiotensin II
- anthrax vaccine
- aprocitentan
- arformoterol inhaled
- armodafinil
- atogepant
- atomoxetine
- atropine ophthalmic
- axitinib
- azilsartan medoxomil
- benazepril
- benzphetamine
- betamethasone
- bevacizumab
- bismuth subsalicylate
- budesonide
- bumetanide
- bupropion
- caffeine
- caffeine citrate
- candesartan cilexetil
- cannabis
- captopril
- celecoxib
- chikungunya vaccine
- chlorothiazide
- chlorthalidone
- clevidipine
- clomipramine
- cocaine
- cortisone
- COVID-19 vaccine
- darbepoetin alfa
- deflazacort
- desmopressin
- desvenlafaxine
- dexamethasone
- dexmethylphenidate
- dextroamphetamine
- diclofenac
- diclofenac topical
- diethylpropion
- diflunisal
- dihydroergotamine
- diphtheria/tetanus vaccine
- diphtheria/tetanus/pertussis vaccine
- dobutamine
- dopamine
- doxapram
- doxazosin
- doxepin
- dronabinol
- droxidopa
- ebola vaccine, live
- eletriptan
- enalapril
- enalaprilat
- enzalutamide
- ephedrine injection
- ephedrine oral
- epinephrine
- eplerenone
- epoetin alfa
- eptinezumab
- erenumab
- ergotamine
- esketamine
- estetrol (contraceptive)
- estradiol (contraceptive)
- ethacrynic acid
- ethinyl estradiol (contraceptive)
- etodolac
- felodipine
- fenfluramine
- fenoldopam
- fenoprofen
- fludrocortisone
- flurbiprofen
- formoterol inhaled
- fosinopril
- fostamatinib
- fremanezumab
- frovatriptan
- galcanezumab
- Haemophilus b vaccine
- hepatitis A vaccine
- hepatitis B vaccine
- hoodia
- human papillomavirus vaccine
- hydralazine
- hydrochlorothiazide
- hydrocortisone
- ibuprofen
- imipramine
- indapamide
- indomethacin
- influenza H5N1 vaccine
- influenza vaccine
- irbesartan
- isradipine
- Japanese encephalitis vaccine
- ketamine
- ketoprofen
- ketorolac
- lenvatinib
- levalbuterol inhaled
- levomilnacipran
- licorice
- linezolid
- lisdexamfetamine
- lisinopril
- losartan
- lumacaftor/ivacaftor
- luspatercept
- magnesium salicylate
- meclofenamate
- mefenamic acid
- meloxicam
- meningococcal vaccine
- methamphetamine
- methoxy polyethylene glycol-epoetin beta
- methyldopa
- methylergonovine
- methylphenidate
- methylprednisolone
- metoclopramide
- metolazone
- milnacipran
- minoxidil
- mirabegron
- modafinil
- moexipril
- nabumetone
- naproxen
- naratriptan
- naxitamab
- nicardipine
- nifedipine
- nimodipine
- niraparib
- nisoldipine
- norepinephrine
- nortriptyline
- olmesartan medoxomil
- olodaterol inhaled
- osilodrostat
- oxaprozin
- oxymetazoline nasal
- oxymetazoline topical
- oxytocin
- pazopanib
- perindopril
- pexidartinib
- phendimetrazine
- phenoxybenzamine
- phentermine
- phentolamine
- phenylephrine
- phenylephrine injection
- phenylephrine nasal
- phenylephrine ophthalmic
- phenylephrine rectal
- piroxicam
- pneumococcal vaccine
- poliovirus vaccine
- pralsetinib
- prazosin
- prednisolone
- prednisone
- protriptyline
- pseudoephedrine
- quetiapine
- quinapril
- ramipril
- ramucirumab
- respiratory syncytial virus vaccine
- rimegepant
- ripretinib
- rizatriptan
- ropinirole
- rotigotine transdermal
- salmeterol inhaled
- salsalate
- sipuleucel-T
- smallpox/mpox vaccine, live
- solriamfetol
- sorafenib
- spironolactone
- sulindac
- sumatriptan
- sunitinib
- tagraxofusp
- telmisartan
- terazosin
- terbutaline
- testosterone
- tetrahydrozoline ophthalmic
- tick-borne encephalitis vaccine
- tivozanib
- tolmetin
- torsemide
- trametinib
- trandolapril
- triamcinolone
- triamterene
- trimipramine
- typhoid vaccine
- ubrogepant
- vadadustat
- valsartan
- vamorolone
- vasopressin
- venlafaxine
- vilanterol inhaled
- viloxazine
- yohimbe
- zavegepant
- ziv-aflibercept
- zolmitriptan
Caution Advised
- beclomethasone inhaled
- beclomethasone nasal
- bosentan
- budesonide inhaled
- budesonide nasal
- budesonide rectal
- butalbital
- cenobamate
- dabrafenib
- dexamethasone ophthalmic
- difluprednate ophthalmic
- etravirine
- flunisolide nasal
- fluocinolone intravitreal
- fluorometholone ophthalmic
- fluticasone furoate
- fluticasone propionate
- hydrocortisone ophthalmic
- lifileucel
- loteprednol ophthalmic
- mavacamten
- mitapivat
- mitotane
- mometasone implant
- mometasone inhaled
- mometasone nasal
- nadofaragene firadenovec intravesical
- nafcillin
- pentobarbital
- phenobarbital
- prednisolone ophthalmic
- primidone
- repotrectinib
- rifabutin
- rifapentine
- sotorasib
- St. John's wort
- tuberculin purified protein derivative
Adverse Reactions .
Serious Reactions
- bradyarrhythmia
- AV block
- infection, serious
- PML
- PML-assoc. immune reconstitution syndrome after D/C
- posterior reversible encephalopathy syndrome
- macular edema
- hepatic injury
- skin CA
Common Reactions
- infection
- headache
- LFTs elevated
- lymphopenia
- dizziness
- arthralgia
- nausea
- HTN
- UTI
- hypercholesterolemia
- bradycardia
- herpes viral infection
- visual acuity decr.
- pulmonary fxn decr.
Safety/Monitoring .
Monitoring Parameters
ALT, AST, bilirubin, CBC w/ diff at baseline if none w/in 6mo of tx start; ECG at baseline; ophthalmic exam at baseline, then periodically; dermatologic exam at baseline, then periodically, esp. if incr. skin CA risk; BP; s/sx infection during tx and x5wk after D/C; VZV antibody testing at baseline if no varicella or vaccination hx; consider MRI for s/sx PML
Pregnancy/Lactation .
Pregnancy
Clinical Summary
avoid use during pregnancy; inadequate human data available; risk of teratogenicity and embryo-fetal death based on animal data at 5x and 6x MRHD
Pregnancy Registry
enroll pts or encourage pts to enroll in Velsipity Pregnancy Registry at 1-800-616-3791
Individuals of Reproductive Potential
avoid pregnancy by using effective contraception during tx and x1wk after D/C in pts of childbearing potential
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: liver; CYP450: 2C8, 2C9, 3A4 substrate; UGT: substrate (enzymes not defined)
Excretion: feces 82% (11% unchanged), urine 5% (none unchanged); Half-life: 30h
Subclass: Inflammatory Bowel Disease (IBD)
Mechanism of Action
exact mechanism of action unknown; binds to sphingosine 1-phosphate receptors 1, 4, and 5; reduces lymphocyte egress from lymph nodes and migration into intestine
Formulary .
No Formulary Selected
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