Selpercatinib

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

  1. abdominal pain
  2. abdominal pain
  3. arthralgia
  4. asthenia
  5. bleeding
  6. bleeding
  7. constipation
  8. constipation
  9. cough
  10. diarrhea
  11. diarrhea
  12. dyspnea
  13. dyspnea
  14. ecchymosis
  15. edema
  16. edema
  17. elevated hepatic enzymes
  18. elevated hepatic enzymes
  19. epistaxis
  20. fatigue
  21. fatigue
  22. fever
  23. GI bleeding
  24. headache
  25. headache
  26. hematemesis
  27. hematoma
  28. hematuria
  29. hemoptysis
  30. hepatotoxicity
  31. hyperbilirubinemia
  32. hyperbilirubinemia
  33. hypercholesterolemia
  34. hyperglycemia
  35. hyperkalemia
  36. hypertension
  37. hypertension
  38. hypoalbuminemia
  39. hypoalbuminemia
  40. hypocalcemia
  41. hypoglycemia
  42. hypomagnesemia
  43. hyponatremia
  44. hypothyroidism
  45. impaired wound healing
  46. infection
  47. intracranial bleeding
  48. leukopenia
  49. maculopapular rash
  50. malaise
  51. melena
  52. myalgia
  53. nausea
  54. nausea
  55. ocular hemorrhage
  56. peripheral edema
  57. petechiae
  58. purpura
  59. QT prolongation
  60. QT prolongation
  61. rash
  62. rash
  63. thrombocytopenia
  64. vaginal bleeding
  65. vomiting
  66. vomiting
  67. 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
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