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Isturisa
osilodrostat
Adult Dosing .
Dosage forms: TAB: 1 mg, 5 mg
Cushing syndrome
- [2-7 mg PO bid]
- Start: 2 mg PO bid, then may incr. dose by 2-4 mg/day no more frequently than q2wk; Max: 60 mg/day; Info: for pts ineligible for or who have failed surgery; adjust dose based on tx response and urinary free cortisol levels; in pts w/ elevated cortisol levels receiving 10 mg bid, may further incr. dose by 10 mg/day no more frequently than q2wk
renal dosing
- [see below]
- renal impairment: no adjustment; Info: reduced urine free cortisol excretion if mod-severe renal impairment; adjust dose based on urine free cortisol levels
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B: start 1 mg bid; Child-Pugh Class C: start 1 mg qhs
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- electrolyte abnormalities, uncorrected
- avoid: breastfeeding during tx and x1wk after D/C
- caution: renal impairment, moderate-severe
- caution: hepatic impairment
- caution: QT prolongation
- caution: QT prolongation family hx
- caution: long QT syndrome, congenital
- caution: torsades de pointes hx
- caution: ventricular arrhythmia
- caution: bradycardia
- caution: MI, recent
- caution: CHF
- caution: hypocortisolism risk
Drug Interactions .
Overview
osilodrostat
cortisol synthesis inhibitor
- CYP2B6 substrate
- CYP3A4 substrate
- CYP1A2 inhibitor, moderate
- CYP2C19 inhibitor, weak
- CYP2D6 inhibitor, weak
- CYP3A4 inhibitor, weak
- hypertensive effects
- hypokalemia
- prolongs QT interval (conditional)
Contraindicated
- cisapride
- fezolinetant
- pimozide
- thioridazine
Avoid/Use Alternative
- alosetron
- alprazolam
- arsenic trioxide
- bedaquiline
- bendamustine
- codeine
- colchicine
- crizotinib
- dihydrocodeine
- domperidone
- dronedarone
- eliglustat
- ephedra
- eribulin
- fexinidazole
- furosemide
- hydrocodone
- hydroxychloroquine
- lefamulin
- lonafarnib
- meperidine
- methadone
- midodrine
- mobocertinib
- oxycodone
- pirfenidone
- pralsetinib
- propafenone
- quizartinib
- simvastatin
- sotalol
- tizanidine
- toremifene
- tramadol
- vorasidenib
- ziprasidone
Monitor/Modify Tx
- abemaciclib
- abiraterone acetate
- acalabrutinib
- acebutolol
- acetazolamide
- adagrasib
- albuterol
- albuterol inhaled
- alfentanil
- aliskiren
- almotriptan
- aloe
- amiloride
- aminophylline
- amiodarone
- amlodipine
- amphetamine
- amphotericin
- anagrelide
- angiotensin II
- apalutamide
- apomorphine
- aprepitant
- aprocitentan
- arformoterol inhaled
- armodafinil
- artemether/lumefantrine
- asciminib
- asenapine
- asparaginase
- atazanavir
- atenolol
- atomoxetine
- atropine ophthalmic
- avacopan
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- avapritinib
- axitinib
- azilsartan medoxomil
- azithromycin
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- benzphetamine
- berotralstat
- betamethasone
- betaxolol
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- bisoprolol
- bosentan
- brexucabtagene autoleucel
- brigatinib
- budesonide
- bumetanide
- bupropion
- butalbital
- cabozantinib
- caffeine
- caffeine citrate
- candesartan cilexetil
- cannabis
- capivasertib
- captopril
- carbamazepine
- carboplatin
- carfilzomib
- carvedilol
- celecoxib
- ceritinib
- cetuximab
- chloramphenicol
- chloroquine
- chlorothiazide
- chlorthalidone
- ciprofloxacin
- cisplatin
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- cocaine
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- darunavir
- decitabine
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- dexamethasone
- dexmedetomidine
- dexmedetomidine injection
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- dextroamphetamine
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- emapalumab
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- ephedrine injection
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- erenumab
- ergotamine
- erythromycin
- esketamine
- esmolol
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- estradiol (contraceptive)
- ethacrynic acid
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- etodolac
- etrasimod
- everolimus
- fedratinib
- felodipine
- fenfluramine
- fenoldopam
- fenoprofen
- fentanyl
- finerenone
- fingolimod
- flecainide
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- fludrocortisone
- fluorouracil
- flurbiprofen
- formoterol inhaled
- fosamprenavir
- foscarnet
- fosinopril
- fosphenytoin
- fostamatinib
- frovatriptan
- fruquintinib
- gepirone
- gilteritinib
- glasdegib
- goserelin
- grapefruit
- guanfacine
- haloperidol
- histrelin
- hoodia
- hydralazine
- hydrochlorothiazide
- hydrocortisone
- hydroxyzine
- ibrutinib
- ibuprofen
- ibutilide
- idelalisib
- imatinib
- imipramine
- indapamide
- indomethacin
- infigratinib
- inotuzumab ozogamicin
- insulin
- irbesartan
- isavuconazonium
- isoflurane
- isoproterenol
- isradipine
- itraconazole
- ivabradine
- ivosidenib
- ixabepilone
- ketamine
- ketoconazole
- ketoprofen
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- labetalol
- leflunomide
- lemborexant
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- lenalidomide
- lenvatinib
- letermovir
- leuprolide
- levalbuterol inhaled
- levofloxacin
- levoketoconazole
- levomilnacipran
- licorice
- lidocaine
- lisdexamfetamine
- lisinopril
- lofexidine
- lomitapide
- lopinavir/ritonavir
- lorlatinib
- losartan
- lovastatin
- lumacaftor/ivacaftor
- lumateperone
- lurasidone
- lurbinectedin
- luspatercept
- macimorelin
- magnesium citrate
- magnesium salicylate
- mavacamten
- meclofenamate
- mefenamic acid
- meloxicam
- methamphetamine
- methazolamide
- methoxy polyethylene glycol-epoetin beta
- methyldopa
- methylergonovine
- methylphenidate
- methylprednisolone
- metoclopramide
- metolazone
- metoprolol
- midazolam
- mifepristone
- milnacipran
- minoxidil
- mirabegron
- mitotane
- modafinil
- moexipril
- motixafortide
- moxifloxacin
- nabumetone
- nadolol
- nafcillin
- naproxen
- naratriptan
- naxitamab
- nebivolol
- necitumumab
- nefazodone
- nelfinavir
- netupitant
- nicardipine
- nifedipine
- nilotinib
- nimodipine
- niraparib
- nirogacestat
- nisoldipine
- norepinephrine
- nortriptyline
- oliceridine
- olmesartan medoxomil
- olodaterol inhaled
- ondansetron
- osimertinib
- oxaprozin
- oxymetazoline nasal
- oxytocin
- ozanimod
- pacritinib
- paliperidone
- palonosetron
- panitumumab
- panobinostat
- pasireotide
- pazopanib
- pemigatinib
- pentamidine
- pentobarbital
- perindopril
- pexidartinib
- phendimetrazine
- phenobarbital
- phenoxybenzamine
- phentermine
- phentolamine
- phenylephrine
- phenylephrine injection
- phenylephrine nasal
- phenylephrine ophthalmic
- phenylephrine rectal
- phenytoin
- pindolol
- piroxicam
- polyethylene glycol
- polyethylene glycol/electrolytes
- pomalidomide
- ponatinib
- ponesimod
- posaconazole
- prazosin
- prednisolone
- prednisone
- primidone
- procainamide
- propranolol
- protriptyline
- pseudoephedrine
- quetiapine
- quinapril
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- quinine
- ramipril
- ramucirumab
- rasagiline
- red yeast rice
- regorafenib
- revumenib
- ribociclib
- rifabutin
- rifampin
- rifapentine
- ripretinib
- ritonavir
- rizatriptan
- romidepsin
- ropinirole
- rucaparib
- sacituzumab govitecan
- salmeterol inhaled
- selinexor
- selpercatinib
- selumetinib
- sevoflurane
- siponimod
- sirolimus
- sirolimus albumin-bound
- sodium benzoate
- sodium phenylacetate
- sodium phenylbutyrate
- sodium polystyrene sulfonate
- sodium thiosulfate
- solriamfetol
- sorafenib
- spironolactone
- St. John's wort
- sufentanil
- sulfate bowel prep
- sulindac
- sumatriptan
- sunitinib
- tacrolimus
- tadalafil
- tafasitamab
- tagraxofusp
- telavancin
- telmisartan
- temsirolimus
- terazosin
- terbutaline
- teriflunomide
- testosterone
- tetrabenazine
- theophylline
- timolol
- tipranavir
- tivozanib
- tolmetin
- tolvaptan
- topiramate
- torsemide
- trametinib
- trandolapril
- trastuzumab
- triamcinolone
- triamterene
- triclabendazole
- trifluridine
- trimipramine
- triptorelin
- tucatinib
- ubrogepant
- vadadustat
- valsartan
- vamorolone
- vandetanib
- vardenafil
- vasopressin
- vemurafenib
- venetoclax
- venlafaxine
- verapamil
- vilanterol inhaled
- viloxazine
- vinblastine
- vincristine
- vinorelbine
- voclosporin
- voriconazole
- warfarin
- yohimbe
- zanubrutinib
- ziv-aflibercept
- zolmitriptan
- zonisamide
Caution Advised
- abrocitinib
- cariprazine
- carisoprodol
- clopidogrel
- cobimetinib
- cyclophosphamide
- daridorexant
- duloxetine
- melatonin
- palovarotene
- perphenazine
- ramelteon
- repotrectinib
- riluzole
- roflumilast
- roflumilast topical
- sirolimus topical
- triazolam
Adverse Reactions .
Serious Reactions
- hypocortisolism
- adrenal insufficiency
- QT prolongation
Common Reactions
- adrenal insufficiency
- fatigue
- nausea
- hypocortisolism
- headache
- edema
- nasopharyngitis
- vomiting
- arthralgia
- back pain
- rash
- diarrhea
- corticotropin incr.
- dizziness
- abdominal pain
- hypokalemia
- myalgia
- appetite decr.
- hypotension
- UTI
- testosterone incr.
- fever
- anemia
- cough
- HTN
- influenza
- hirsutism
- acne
- dyspepsia
- insomnia
- anxiety
- depression
- gastroenteritis
- malaise
- tachycardia
- alopecia
- ALT or AST incr.
- QT prolongation
Safety/Monitoring .
Monitoring Parameters
K, Mg at baseline; ECG at baseline, w/in 1wk of tx start, then as clinically indicated or more frequently if QT prolongation risk; adrenal function if hepatic impairment
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; no known risk of teratogenicity based on animal data at doses up to 8x MRHD
Lactation
Clinical Summary
avoid breastfeeding during tx and x1wk after D/C; no human data available, though theoretical risk of infant adrenal insufficiency based on drug's mechanism of action; no human data available to assess effects on milk production
Pharmacology .
Metabolism: liver; CYP450: 2B6, 2D6, 3A4 substrate; UGT: substrate (enzymes not defined)
Excretion: urine 90.6% (5.2% unchanged), feces 1.6%; Half-life: 4h
Subclass: Cushing Syndrome
Mechanism of Action
inhibits 11 beta-hydroxylase (CYP11B1), blocking cortisol biosynthesis
Formulary .
No Formulary Selected
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