Avapritinib Brand Name– AYVAKIT
What is Avapritinib
Avapritinib is a tyrosine kinase inhibitor targeting platelet-derived growth factor receptor alpha (PDGFRA) and PDGFRA D842 mutations as well as multiple KIT exon 11, 11/17, and 17 mutations.
It is indicated for the treatment of adults with unresectable or metastatic gastrointestinal stromal tumor (GIST) harboring a PDGFRA exon 18 mutation, including PDGFRA D842V mutations.
Central nervous system adverse reactions including cognitive impairment, dizziness, sleep disorders, mood disorders, speech disorders, and hallucinations occur in more than half of patients treated with avapritinib and may require an interruption of therapy or dose reduction.
Coadministration of certain drugs may need to be avoided or dosage adjustments may be necessary; review drug interactions.
Indications
- gastrointestinal stromal tumors (GIST)
For the treatment of gastrointestinal stromal tumors (GIST)
NOTE: The FDA has designated avapritinib as an orphan drug for this indication.
for the treatment of unresectable or metastatic gastrointestinal stromal tumors (GIST) with platelet-derived growth factor-alpha (PDGFRA) exon 18 mutation, including PDGFRA D842V mutations
Side Effects
- abdominal pain
- agitation
- alopecia
- amnesia
- anemia
- anorexia
- anxiety
- asthenia
- confusion
- constipation
- dementia
- depression
- diarrhea
- dizziness
- dysarthria
- dysgeusia
- dyspepsia
- dysphoria
- dyspnea
- edema
- elevated hepatic enzymes
- encephalopathy
- fatigue
- fever
- GI bleeding
- hair discoloration
- hallucinations
- headache
- hyperbilirubinemia
- hypertension
- hyperthyroidism
- hypoalbuminemia
- hypokalemia
- hypomagnesemia
- hyponatremia
- hypophosphatemia
- hypothyroidism
- impaired cognition
- infection
- insomnia
- intracranial bleeding
- irritability
- lacrimation
- leukopenia
- maculopapular rash
- memory impairment
- nausea
- neutropenia
- palmar-plantar erythrodysesthesia (hand and foot syndrome)
- peripheral edema
- pleural effusion
- prolonged bleeding time
- rash
- renal failure (unspecified)
- stroke
- subdural hematoma
- testicular swelling
- thrombocytopenia
- vomiting
- weight loss
Monitoring Parameters
- pregnancy testing
Contraindications
- anxiety
- breast-feeding
- contraception requirements
- dementia
- depression
- infertility
- male-mediated teratogenicity
- mental status changes
- pregnancy
- pregnancy testing
- reproductive risk
- stroke
Interactions
- Acetaminophen; Butalbital
- Acetaminophen; Butalbital; Caffeine
- Acetaminophen; Butalbital; Caffeine; Codeine
- Amiodarone
- Amobarbital
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Apalutamide
- Aprepitant, Fosaprepitant
- Aspirin, ASA; Butalbital; Caffeine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Atazanavir
- Atazanavir; Cobicistat
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Bexarotene
- Bosentan
- Brigatinib
- Butabarbital
- Carbamazepine
- Cenobamate
- Ceritinib
- Chloramphenicol
- Ciprofloxacin
- Clarithromycin
- Cobicistat
- Conivaptan
- Crizotinib
- Cyclosporine
- Dabrafenib
- Danazol
- Darunavir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Delavirdine
- Dexamethasone
- Diltiazem
- Dronedarone
- Duvelisib
- Efavirenz
- Efavirenz; Emtricitabine; Tenofovir
- Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
- Elagolix
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Enzalutamide
- Erythromycin
- Erythromycin; Sulfisoxazole
- Eslicarbazepine
- Etravirine
- Fedratinib
- Fluconazole
- Fluvoxamine
- Fosamprenavir
- Fosphenytoin
- grapefruit juice
- Idelalisib
- Imatinib
- Indinavir
- Isavuconazonium
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Itraconazole
- Ketoconazole
- Lefamulin
- Letermovir
- Lopinavir; Ritonavir
- Lorlatinib
- Lumacaftor; Ivacaftor
- Lumacaftor; Ivacaftor
- Mephobarbital
- Methohexital
- Mifepristone
- Mitotane
- Modafinil
- Nafcillin
- Nefazodone
- Nelfinavir
- Netupitant, Fosnetupitant; Palonosetron
- Nevirapine
- Nilotinib
- Ombitasvir; Paritaprevir; Ritonavir
- Omeprazole; Amoxicillin; Rifabutin
- Pentobarbital
- Phenobarbital
- Phenytoin
- Posaconazole
- Primidone
- Ribociclib
- Ribociclib; Letrozole
- Rifabutin
- Rifampin
- Rifapentine
- Rifaximin
- Ritonavir
- Saquinavir
- Secobarbital
- St. John’s Wort, Hypericum perforatum
- Telithromycin
- Thiopental
- Tipranavir
- Trandolapril; Verapamil
- Tucatinib
- Verapamil
- Voriconazole
