Osilodrostat Brand Name– ISTURISA
What is Osilodrostat
Osilodrostat in an oral cortisol synthesis inhibitor that works by inhibiting steroid 11-beta-hydroxylase (also known as CYP11B1), an enzyme responsible for the final step of cortisol biosynthesis in the adrenal gland.
Osilodrostat is used to treat adult patients with Cushing’s disease who cannot be treated with surgery, or in whom surgery is ineffective.
Osilodrostat was studied in 137 adult patients (the majority of whom either had undergone pituitary surgery that did not cure Cushing’s disease or were not surgical candidates); at the end of the single-arm, open-label 24-week period, about half of patients had cortisol levels within normal limits.
After this point, 71 patients who were taking stable doses and had tolerated the drug for the last 12 weeks entered an 8-week, double-blind, randomized withdrawal study; at the end of this withdrawal period, 86% of patients receiving osilodrostat had maintained cortisol levels within normal limits compared to 30% of patients taking the placebo.
The most serious side effect of the drug is adrenal insufficiency.
Hypocortisolism, QTc interval prolongation, and elevations in adrenal hormone precursors may also occur in patients taking osilodrostat.
The FDA approved osilodrostat in March 2020.
Indications
- Cushing’s syndrome
For the treatment of Cushing’s syndrome in patients for whom pituitary surgery is not an option or has not been curative
Side Effects
- abdominal pain
- acne vulgaris
- adrenocortical insufficiency
- alopecia
- anemia
- anxiety
- arthralgia
- back pain
- cough
- depression
- diarrhea
- dizziness
- dyspepsia
- edema
- elevated hepatic enzymes
- fatigue
- headache
- hirsutism
- hypertension
- hypertrichosis
- hypoglycemia
- hypokalemia
- hypotension
- infection
- influenza
- insomnia
- malaise
- myalgia
- nausea
- neutropenia
- pharyngitis
- QT prolongation
- rash
- sinus tachycardia
- syncope
- vomiting
Monitoring Parameters
- blood pressure
- ECG
- serum cortisol
- serum magnesium
- serum potassium
- urinary free cortisol
Contraindications
- acne vulgaris
- adrenal insufficiency
- apheresis
- AV block
- bradycardia
- breast-feeding
- cardiac arrhythmias
- cardiomyopathy
- celiac disease
- children
- edema
- electrolyte imbalance
- females
- fever
- geriatric
- heart failure
- hepatic disease
- human immunodeficiency virus (HIV) infection
- hyperparathyroidism
- hypertension
- hypocalcemia
- hypokalemia
- hypomagnesemia
- hypothermia
- hypothyroidism
- infants
- long QT syndrome
- myocardial infarction
- pheochromocytoma
- pregnancy
- QT prolongation
- renal impairment
- rheumatoid arthritis
- sickle cell disease
- sleep deprivation
- stroke
- systemic lupus erythematosus (SLE)
Interactions
- Acetaminophen; Butalbital; Caffeine; Codeine
- Acetaminophen; Caffeine; Dihydrocodeine
- Acetaminophen; Codeine
- Acetaminophen; Hydrocodone
- Acetaminophen; Oxycodone
- Acetaminophen; Tramadol
- Aclidinium; Formoterol
- Albuterol
- Albuterol; Ipratropium
- Alfentanil
- Alfuzosin
- Amiodarone
- Amitriptyline
- Amitriptyline; Chlordiazepoxide
- Amoxapine
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Anagrelide
- Apalutamide
- Apomorphine
- Arformoterol
- Aripiprazole
- Arsenic Trioxide
- Artemether; Lumefantrine
- Asenapine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Aspirin, ASA; Caffeine; Dihydrocodeine
- Aspirin, ASA; Carisoprodol; Codeine
- Aspirin, ASA; Oxycodone
- Atazanavir
- Atazanavir; Cobicistat
- Atomoxetine
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Azithromycin
- Bedaquiline
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Benzhydrocodone; Acetaminophen
- Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
- Bismuth Subsalicylate; Metronidazole; Tetracycline
- Brompheniramine; Guaifenesin; Hydrocodone
- Brompheniramine; Hydrocodone; Pseudoephedrine
- Budesonide; Formoterol
- Bupivacaine; Lidocaine
- Buprenorphine
- Buprenorphine; Naloxone
- Carbamazepine
- Carbinoxamine; Hydrocodone; Phenylephrine
- Carbinoxamine; Hydrocodone; Pseudoephedrine
- Ceritinib
- Chloramphenicol
- Chloroquine
- Chlorpheniramine; Codeine
- Chlorpheniramine; Dihydrocodeine; Phenylephrine
- Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
- Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
- Chlorpheniramine; Hydrocodone
- Chlorpheniramine; Hydrocodone; Phenylephrine
- Chlorpheniramine; Hydrocodone; Pseudoephedrine
- Chlorpromazine
- Ciprofloxacin
- Cisapride
- Citalopram
- Clarithromycin
- Clofazimine
- Clomipramine
- Clozapine
- Cobicistat
- Codeine
- Codeine; Guaifenesin
- Codeine; Phenylephrine; Promethazine
- Codeine; Promethazine
- Conivaptan
- Crizotinib
- Cyclosporine
- Darunavir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Dasatinib
- Degarelix
- Delavirdine
- Desflurane
- Desipramine
- Deutetrabenazine
- Dextromethorphan; Promethazine
- Dextromethorphan; Quinidine
- Dihydrocodeine; Guaifenesin; Pseudoephedrine
- Diphenhydramine; Hydrocodone; Phenylephrine
- Disopyramide
- Dofetilide
- Dolasetron
- Dolutegravir; Rilpivirine
- Donepezil
- Donepezil; Memantine
- Doxepin
- Dronedarone
- Droperidol
- Efavirenz
- Efavirenz; Emtricitabine; Tenofovir
- Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
- Eliglustat
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Emtricitabine; Rilpivirine; Tenofovir alafenamide
- Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
- Enalapril; Felodipine
- Encorafenib
- Enflurane
- Entrectinib
- Enzalutamide
- Eribulin
- Erlotinib
- Erythromycin
- Erythromycin; Sulfisoxazole
- Escitalopram
- Ezogabine
- Felodipine
- Fentanyl
- Fingolimod
- Flecainide
- Flibanserin
- Fluconazole
- Fluoxetine
- Fluoxetine; Olanzapine
- Fluphenazine
- Fluticasone; Salmeterol
- Fluticasone; Umeclidinium; Vilanterol
- Fluticasone; Vilanterol
- Fluvoxamine
- Formoterol
- Formoterol; Mometasone
- Fosamprenavir
- Foscarnet
- Fosphenytoin
- Gemifloxacin
- Gemtuzumab Ozogamicin
- Gilteritinib
- Glasdegib
- Glycopyrrolate; Formoterol
- Goserelin
- Granisetron
- grapefruit juice
- Guaifenesin; Hydrocodone
- Guaifenesin; Hydrocodone; Pseudoephedrine
- Halogenated Anesthetics
- Haloperidol
- Halothane
- Histrelin
- Homatropine; Hydrocodone
- Hydrochlorothiazide, HCTZ; Propranolol
- Hydrocodone
- Hydrocodone; Ibuprofen
- Hydrocodone; Phenylephrine
- Hydrocodone; Potassium Guaiacolsulfonate
- Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
- Hydrocodone; Pseudoephedrine
- Hydroxychloroquine
- Hydroxyzine
- Ibuprofen; Oxycodone
- Ibutilide
- Idelalisib
- Iloperidone
- Imipramine
- Indacaterol
- Indacaterol; Glycopyrrolate
- Indinavir
- Inotuzumab Ozogamicin
- Isoflurane
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Isradipine
- Itraconazole
- Ivosidenib
- Ixabepilone
- Ketoconazole
- Lapatinib
- Lefamulin
- Lemborexant
- Lenvatinib
- Leuprolide
- Leuprolide; Norethindrone
- Levalbuterol
- Levofloxacin
- Lidocaine
- Lidocaine; Prilocaine
- Lithium
- Lofexidine
- Lomitapide
- Long-acting beta-agonists
- Loperamide
- Loperamide; Simethicone
- Lopinavir; Ritonavir
- Lumacaftor; Ivacaftor
- Lumacaftor; Ivacaftor
- Macimorelin
- Maprotiline
- Mefloquine
- Meperidine; Promethazine
- Metaproterenol
- Methadone
- Metronidazole
- Mexiletine
- Midostaurin
- Mifepristone
- Mirtazapine
- Mitotane
- Moxifloxacin
- Nefazodone
- Nelfinavir
- Nilotinib
- Nimodipine
- Nisoldipine
- Nortriptyline
- Octreotide
- Ofloxacin
- Olanzapine
- Olodaterol
- Ombitasvir; Paritaprevir; Ritonavir
- Ondansetron
- Osimertinib
- Oxaliplatin
- Oxycodone
- Ozanimod
- Paliperidone
- Panobinostat
- Pasireotide
- Pazopanib
- Pentamidine
- Perphenazine
- Perphenazine; Amitriptyline
- Phenobarbital
- Phenylephrine; Promethazine
- Phenytoin
- Pimavanserin
- Pimozide
- Pirbuterol
- Pirfenidone
- Pitolisant
- Posaconazole
- Primaquine
- Primidone
- Procainamide
- Prochlorperazine
- Promethazine
- Propafenone
- Propranolol
- Protriptyline
- Quetiapine
- Quinidine
- Quinine
- Ramelteon
- Ranolazine
- Rasagiline
- Ribociclib
- Ribociclib; Letrozole
- Rifampin
- Rilpivirine
- Risperidone
- Ritonavir
- Romidepsin
- Salmeterol
- Saquinavir
- Selpercatinib
- Sertraline
- Sevoflurane
- Short-acting beta-agonists
- Siponimod
- Sirolimus
- Solifenacin
- Sorafenib
- Sotalol
- St. John’s Wort, Hypericum perforatum
- Sufentanil
- Sunitinib
- Tacrolimus
- Tamoxifen
- Telavancin
- Telithromycin
- Terbutaline
- Tetrabenazine
- Theophylline, Aminophylline
- Thioridazine
- Tiotropium; Olodaterol
- Tizanidine
- Tolterodine
- Toremifene
- Tramadol
- Trazodone
- Triclabendazole
- Trifluoperazine
- Trimipramine
- Triptorelin
- Tucatinib
- Ubrogepant
- Umeclidinium; Vilanterol
- Vandetanib
- Vardenafil
- Vemurafenib
- Venlafaxine
- Voriconazole
- Vorinostat
- Warfarin
- Ziprasidone
