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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 patients ineligible for or who have failed surgery; adjust dose based on tx response and urinary free cortisol levels; in patients with 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 moderate-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 history
- caution: long QT syndrome, congenital
- caution: torsades de pointes history
- 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
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- hypocortisolism
- adrenal insufficiency
- QT prolongation
- neutropenia
Common Reactions
- adrenal insufficiency
- fatigue
- appetite decr.
- nausea
- arthralgia
- hypocortisolism
- headache
- myalgia
- edema
- diarrhea
- nasopharyngitis
- vomiting
- dizziness
- hypokalemia
- back pain
- rash
- hypotension
- tachycardia
- HTN
- corticotropin incr.
- abdominal pain
- QT prolongation
- UTI
- pruritus
- testosterone incr.
- fever
- anemia
- cough
- influenza
- viral infection
- hirsutism
- acne
- dyspepsia
- insomnia
- anxiety
- depression
- gastroenteritis
- malaise
- neutropenia
- alopecia
- ALT or AST incr.
Safety/Monitoring .
Monitoring Parameters
K, Mg at baseline; ECG at baseline, within 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: for osilodrostat: liver; CYP450: 2B6, 2D6, 3A4 substrate; UGT: substrate (enzymes not defined)
Excretion: for osilodrostat: urine 90.6% (5.2% unchanged), feces 1.6%; Half-life: 4h
Subclass: Cushing Syndrome
Mechanism of Action
for osilodrostat: inhibits 11 beta-hydroxylase (CYP11B1), blocking cortisol biosynthesis
Formulary .
No Formulary Selected
Manufacturer/Pricing .
Manufacturer: Recordati Rare Diseases Inc.
DEA/FDA: Rx
Retail Price
Estimated prices only. For current pricing, visit GoodRx.
oral tablet:
- 1 mg (1 carton, 20 tablets): $2,578.00
- 5 mg (1 carton, 20 tablets): $8,835.00
- 10 mg (1 carton, 20 tablets): $10,489.00
oral tablet:
- 1 mg (1 carton, 3 blister packs of 20 tablets): $7,714.00
- 5 mg (1 carton, 3 blister packs of 20 tablets): $26,485.00
- 10 mg (1 carton, 3 blister packs of 20 tablets): $31,449.00
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