What is Selpercatinib
Selpercatinib is a kinase inhibitor that targets wild-type RET and multiple mutated RET isoforms.
It is indicated for the treatment of adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC), adult and pediatric patients 12 years of age and older with advanced or metastatic RET-mutant medullary thyroid cancer who require systemic therapy, and adult and pediatric patients 12 years of age and older with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate).
Brand Name
Retevmo
Indications & Dosage
- non-small cell lung cancer (NSCLC)
- thyroid cancer
For the treatment of non-small cell lung cancer (NSCLC)
NOTE: Selpercatinib is designated by the FDA as an orphan drug for this indication.
for the treatment of metastatic RET fusion-positive non-small cell lung cancer (NSCLC)
Side Effects
- abdominal pain
- abdominal pain
- arthralgia
- asthenia
- bleeding
- bleeding
- constipation
- constipation
- cough
- diarrhea
- diarrhea
- dyspnea
- dyspnea
- ecchymosis
- edema
- edema
- elevated hepatic enzymes
- elevated hepatic enzymes
- epistaxis
- fatigue
- fatigue
- fever
- GI bleeding
- headache
- headache
- hematemesis
- hematoma
- hematuria
- hemoptysis
- hepatotoxicity
- hyperbilirubinemia
- hyperbilirubinemia
- hypercholesterolemia
- hyperglycemia
- hyperkalemia
- hypertension
- hypertension
- hypoalbuminemia
- hypoalbuminemia
- hypocalcemia
- hypoglycemia
- hypomagnesemia
- hyponatremia
- hypothyroidism
- impaired wound healing
- infection
- intracranial bleeding
- leukopenia
- maculopapular rash
- malaise
- melena
- myalgia
- nausea
- nausea
- ocular hemorrhage
- peripheral edema
- petechiae
- purpura
- QT prolongation
- QT prolongation
- rash
- rash
- thrombocytopenia
- vaginal bleeding
- vomiting
- vomiting
- xerostomia
Monitoring Parameters
- blood pressure
- LFTs
- pregnancy testing
Contraindications
- apheresis
- AV block
- bleeding
- bradycardia
- breast-feeding
- cardiomyopathy
- celiac disease
- contraception requirements
- females
- fever
- geriatric
- heart failure
- hepatic disease
- hepatotoxicity
- human immunodeficiency virus (HIV) infection
- hyperparathyroidism
- hypertension
- hypocalcemia
- hypokalemia
- hypomagnesemia
- hypothermia
- hypothyroidism
- infertility
- long QT syndrome
- male-mediated teratogenicity
- myocardial infarction
- pheochromocytoma
- pregnancy
- pregnancy testing
- QT prolongation
- renal impairment
- reproductive risk
- rheumatoid arthritis
- sickle cell disease
- sleep deprivation
- stroke
- systemic lupus erythematosus (SLE)
Interactions
- Acetaminophen; Butalbital
- Acetaminophen; Butalbital; Caffeine
- Acetaminophen; Butalbital; Caffeine; Codeine
- Acetaminophen; Caffeine; Dihydrocodeine
- Acetaminophen; Codeine
- Acetaminophen; Hydrocodone
- Acetaminophen; Oxycodone
- Acetaminophen; Tramadol
- Aclidinium; Formoterol
- Albuterol
- Albuterol; Ipratropium
- Alfentanil
- Alfuzosin
- Aluminum Hydroxide
- Aluminum Hydroxide; Magnesium Carbonate
- Aluminum Hydroxide; Magnesium Hydroxide
- Aluminum Hydroxide; Magnesium Hydroxide; Simethicone
- Aluminum Hydroxide; Magnesium Trisilicate
- Amiodarone
- Amitriptyline
- Amitriptyline; Chlordiazepoxide
- Amobarbital
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Anagrelide
- Antacids
- Apalutamide
- Apomorphine
- Aprepitant, Fosaprepitant
- Arformoterol
- Aripiprazole
- Arsenic Trioxide
- Artemether; Lumefantrine
- Asenapine
- Aspirin, ASA; Butalbital; Caffeine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Aspirin, ASA; Caffeine; Dihydrocodeine
- Aspirin, ASA; Carisoprodol; Codeine
- Aspirin, ASA; Omeprazole
- Aspirin, ASA; Oxycodone
- Atazanavir; Cobicistat
- Atomoxetine
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Azithromycin
- Bedaquiline
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Benzhydrocodone; Acetaminophen
- Bexarotene
- Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
- Bismuth Subsalicylate; Metronidazole; Tetracycline
- Bosentan
- Brompheniramine; Guaifenesin; Hydrocodone
- Brompheniramine; Hydrocodone; Pseudoephedrine
- Budesonide; Formoterol
- Bupivacaine; Lidocaine
- Buprenorphine
- Buprenorphine; Naloxone
- Butabarbital
- Calcium Carbonate
- Calcium Carbonate; Magnesium Hydroxide
- Calcium Carbonate; Risedronate
- Calcium Carbonate; Simethicone
- Carbamazepine
- Carbinoxamine; Hydrocodone; Phenylephrine
- Carbinoxamine; Hydrocodone; Pseudoephedrine
- Cenobamate
- Ceritinib
- Chloramphenicol
- Chloroquine
- Chlorpheniramine; Codeine
- Chlorpheniramine; Dihydrocodeine; Phenylephrine
- Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
- Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
- Chlorpheniramine; Hydrocodone
- Chlorpheniramine; Hydrocodone; Phenylephrine
- Chlorpheniramine; Hydrocodone; Pseudoephedrine
- Chlorpromazine
- Cimetidine
- Ciprofloxacin
- Cisapride
- Citalopram
- Clarithromycin
- Clofazimine
- Clomipramine
- Clozapine
- Cobicistat
- Codeine
- Codeine; Guaifenesin
- Codeine; Phenylephrine; Promethazine
- Codeine; Promethazine
- Conivaptan
- Crizotinib
- Cyclosporine
- Dabrafenib
- Danazol
- Darunavir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Dasatinib
- Degarelix
- Delavirdine
- Desflurane
- Desipramine
- Deutetrabenazine
- Dexamethasone
- Dexlansoprazole
- Dextromethorphan; Promethazine
- Dextromethorphan; Quinidine
- Diazepam
- Dihydrocodeine; Guaifenesin; Pseudoephedrine
- Diltiazem
- Diphenhydramine; Hydrocodone; Phenylephrine
- Disopyramide
- Dofetilide
- Dolasetron
- Dolutegravir; Rilpivirine
- Donepezil
- Donepezil; Memantine
- Doxepin
- Dronedarone
- Droperidol
- Duvelisib
- Efavirenz
- Efavirenz; Emtricitabine; Tenofovir
- Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
- Elagolix
- Elagolix; Estradiol; Norethindrone acetate
- 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
- Erythromycin
- Erythromycin; Sulfisoxazole
- Escitalopram
- Eslicarbazepine
- Esomeprazole
- Esomeprazole; Naproxen
- Etravirine
- Ezogabine
- Famotidine
- Famotidine; Ibuprofen
- Fedratinib
- Felodipine
- Fentanyl
- Fingolimod
- Flecainide
- Flibanserin
- Fluconazole
- Fluoxetine
- Fluoxetine; Olanzapine
- Fluphenazine
- Flurazepam
- Fluticasone; Salmeterol
- Fluticasone; Umeclidinium; Vilanterol
- Fluticasone; Vilanterol
- Fluvoxamine
- Formoterol
- Formoterol; Mometasone
- Fosamprenavir
- Foscarnet
- Fosphenytoin
- Gemifloxacin
- Gemtuzumab Ozogamicin
- Gilteritinib
- Glasdegib
- Glimepiride; Rosiglitazone
- Glycopyrrolate; Formoterol
- Goserelin
- Granisetron
- grapefruit juice
- Guaifenesin; Hydrocodone
- Guaifenesin; Hydrocodone; Pseudoephedrine
- Halogenated Anesthetics
- Haloperidol
- Halothane
- Histrelin
- Homatropine; Hydrocodone
- Hydrocodone
- Hydrocodone; Ibuprofen
- Hydrocodone; Phenylephrine
- Hydrocodone; Potassium Guaiacolsulfonate
- Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
- Hydrocodone; Pseudoephedrine
- Hydroxychloroquine
- Hydroxyzine
- Ibuprofen; Oxycodone
- Ibutilide
- Idelalisib
- Iloperidone
- Imatinib
- Imipramine
- Indacaterol
- Indacaterol; Glycopyrrolate
- Indinavir
- Inotuzumab Ozogamicin
- Isavuconazonium
- Isoflurane
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Isradipine
- Itraconazole
- Ivosidenib
- Ixabepilone
- Ketoconazole
- Lansoprazole
- Lansoprazole; Naproxen
- Lapatinib
- Lefamulin
- Lemborexant
- Lenvatinib
- Letermovir
- Leuprolide
- Leuprolide; Norethindrone
- Levalbuterol
- Levofloxacin
- Lidocaine
- Lithium
- Lofexidine
- Lomitapide
- Long-acting beta-agonists
- Loperamide
- Loperamide; Simethicone
- Lopinavir; Ritonavir
- Lorlatinib
- Macimorelin
- Magnesium Hydroxide
- Maprotiline
- Mefloquine
- Meperidine; Promethazine
- Metaproterenol
- Metformin; Rosiglitazone
- Methadone
- Methohexital
- Metronidazole
- Midostaurin
- Mifepristone
- Mirtazapine
- Mitotane
- Modafinil
- Moxifloxacin
- Nafcillin
- Nanoparticle Albumin-Bound Paclitaxel
- Nefazodone
- Nelfinavir
- Netupitant, Fosnetupitant; Palonosetron
- Nevirapine
- Nilotinib
- Nimodipine
- Nisoldipine
- Nizatidine
- Nortriptyline
- Octreotide
- Ofloxacin
- Olanzapine
- Olodaterol
- Ombitasvir; Paritaprevir; Ritonavir
- Omeprazole
- Omeprazole; Amoxicillin; Rifabutin
- Omeprazole; Sodium Bicarbonate
- Ondansetron
- Osilodrostat
- Osimertinib
- Oxaliplatin
- Oxycodone
- Ozanimod
- Paliperidone
- Panobinostat
- Pantoprazole
- Pasireotide
- Pazopanib
- Pentamidine
- Perphenazine
- Perphenazine; Amitriptyline
- Phenobarbital
- Phenylephrine; Promethazine
- Phenytoin
- Pimavanserin
- Pimozide
- Pirbuterol
- Pitolisant
- Posaconazole
- Primaquine
- Primidone
- Procainamide
- Prochlorperazine
- Promethazine
- Propafenone
- Protriptyline
- Quetiapine
- Quinidine
- Quinine
- Rabeprazole
- Ranitidine
- Ranolazine
- Ribociclib
- Ribociclib; Letrozole
- Rifabutin
- Rifampin
- Rifapentine
- Rilpivirine
- Risperidone
- Ritonavir
- Romidepsin
- Rosiglitazone
- Salmeterol
- Saquinavir
- Secobarbital
- Selexipag
- Sertraline
- Sevoflurane
- Short-acting beta-agonists
- Siponimod
- Sirolimus
- Solifenacin
- Sorafenib
- Sotalol
- St. John’s Wort, Hypericum perforatum
- Sunitinib
- Tacrolimus
- Tamoxifen
- Telavancin
- Telithromycin
- Terbutaline
- Tetrabenazine
- Thioridazine
- Tiotropium; Olodaterol
- Tolterodine
- Toremifene
- Tramadol
- Trandolapril; Verapamil
- Trazodone
- Triazolam
- Tricyclic antidepressants
- Trifluoperazine
- Trimipramine
- Triptorelin
- Tucatinib
- Ubrogepant
- Umeclidinium; Vilanterol
- Vandetanib
- Vardenafil
- Vemurafenib
- Venlafaxine
- Verapamil
- Vinorelbine
- Voriconazole
- Vorinostat
- Warfarin
- Ziprasidone
