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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 within 6mo
- unstable angina within 6mo
- stroke within 6mo
- TIA within 6mo
- decompensated heart failure with hospitalization within 6mo
- NYHA Class III-IV CHF within 6mo
- AV block, 2nd-3rd degree (patients without pacemaker)
- AV block history, 2nd-3rd degree (patients without pacemaker)
- sick sinus syndrome (patients without pacemaker)
- sick sinus syndrome history (patients without pacemaker)
- sino-atrial block (patients without pacemaker)
- sino-atrial block history (patients without pacemaker)
- phototherapy, concurrent
- avoid: sun exposure
- avoid: UV light exposure, artificial
- caution: patients of childbearing potential
- caution: electrolyte abnormalities
- caution: AV block risk
- caution: bradycardia risk
- caution: QTc >470 msec (female patients)
- caution: QTc >450 msec (male patients)
- caution: long QT syndrome, congenital
- caution: QT prolongation family history
- caution: torsades de pointes history
- 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
- immunomodulatory 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
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- belinostat
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- berotralstat
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- betaxolol ophthalmic
- bimekizumab
- bisoprolol
- blinatumomab
- bortezomib
- brentuximab vedotin
- brexucabtagene autoleucel
- brigatinib
- brodalumab
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- busulfan
- cabazitaxel
- cabozantinib
- canakinumab
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- carvedilol
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- dinutuximab
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- gemfibrozil
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- grapefruit
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- hydroxyzine
- ibritumomab tiuxetan
- ibrutinib
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- icotrokinra
- idarubicin
- idecabtagene vicleucel
- idelalisib
- ifosfamide
- imatinib
- inebilizumab
- infliximab
- inotuzumab ozogamicin
- iptacopan
- irinotecan
- isatuximab
- isavuconazonium
- isoflurane
- itraconazole
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- ivosidenib
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- ixekizumab
- ketoconazole
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- lacosamide
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- lebrikizumab
- lefamulin
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- levobunolol ophthalmic
- levofloxacin
- levoketoconazole
- lidocaine
- linvoseltamab
- lisocabtagene maraleucel
- lithium
- lofexidine
- lomustine
- lonafarnib
- loncastuximab tesirine
- lopinavir/ritonavir
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- lymphocyte immune globulin, anti-thymocyte globulin
- macimorelin
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- natalizumab
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- netupitant
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- octreotide
- ofatumumab
- oliceridine
- ondansetron
- osimertinib
- oxaliplatin
- ozanimod
- paclitaxel
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- palonosetron
- paltusotine
- pasireotide
- pegcetacoplan
- pentamidine
- pentostatin
- phenytoin
- pimecrolimus topical
- pindolol
- pirtobrutinib
- polatuzumab vedotin
- pomalidomide
- ponatinib
- ponesimod
- posaconazole
- pozelimab
- praziquantel
- procainamide
- procarbazine
- propafenone
- propofol
- propranolol
- pyridostigmine
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- quizartinib
- rabies vaccine
- ravulizumab
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- ropeginterferon alfa-2b
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- sarilumab
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- secukinumab
- selinexor
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- sevoflurane
- sibeprenlimab
- siltuximab
- siponimod
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- sirolimus albumin-bound
- sotalol
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- succinylcholine
- sufentanil
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- sulfasalazine
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- ustekinumab
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- 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
- ephedrine injection
- ephedrine oral
- epinephrine
- eplerenone
- epoetin alfa
- eptinezumab
- erenumab
- ergotamine
- esketamine
- estetrol (contraceptive)
- estradiol (contraceptive)
- ethacrynic acid
- ethanol (alcoholic beverage)
- 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
- hydroxocobalamin IV
- 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
- methyltestosterone
- metoclopramide
- metolazone
- milnacipran
- minoxidil
- mirabegron
- modafinil
- moexipril
- nabumetone
- naproxen
- naratriptan
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- nicardipine
- nifedipine
- nimodipine
- niraparib
- nisoldipine
- norepinephrine
- nortriptyline
- olmesartan medoxomil
- olodaterol inhaled
- osilodrostat
- oxaprozin
- oxymetazoline nasal
- 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
- ziftomenib
- ziv-aflibercept
- zolmitriptan
Caution Advised
- beclomethasone inhaled
- beclomethasone nasal
- bosentan
- budesonide inhaled
- budesonide nasal
- budesonide rectal
- butalbital
- cenobamate
- coccidioides immitis skin test antigen
- dabrafenib
- dexamethasone ophthalmic
- difluprednate ophthalmic
- enzalutamide
- 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-associated 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 function decr.
Safety/Monitoring .
Monitoring Parameters
ALT, AST, bilirubin, CBC with diff at baseline if none within 6mo of tx start; ECG at baseline; ophthalmic exam at baseline, then periodically; dermatologic exam at baseline, then periodically, especially if incr. skin CA risk; BP; signs/symptoms of infection during tx and x5wk after D/C; VZV antibody testing at baseline if no varicella or vaccination history; consider MRI for signs/symptoms of 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 patients or encourage patients 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 patients 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: for etrasimod: liver; CYP450: 2C8, 2C9, 3A4 substrate; UGT: substrate (enzymes not defined)
Excretion: for etrasimod: feces 82% (11% unchanged), urine 5% (none unchanged); Half-life: 30h
Subclass: Inflammatory Bowel Disease (IBD)
Mechanism of Action
for etrasimod: 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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