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Aqvesme
mitapivat
Black Box Warnings .
Appropriate Use
restricted distribution program, Aqvesme REMS, due to risk of hepatocellular injury; prescribers, pharmacies, and patients must enroll at 1-800-625-9951 or www.aqvesmerems.com
Hepatocellular Injury
can occur within 6mo of tx; measure LFTs, including ALT, AST, alk phos, and total bilirubin with fractionation, at baseline and q4wk x24wk, then as clinically indicated; avoid tx in patients with cirrhosis; D/C tx if hepatic injury suspected
Adult Dosing .
Dosage forms: TAB: 100 mg
Restricted Distribution in US
- [1-800-625-9951 or www.aqvesmerems.com for more info]
anemia, alpha- or beta-thalassemia-associated
- [100 mg PO bid]
- Info: do not cut/crush/chew/dissolve tab; see pkg insert for dose adjustments based on toxicities
renal dosing
- [see below]
- eGFR >60: no adjustment; eGFR <60: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B or C without cirrhosis: not defined, caution advised; Child-Pugh Class A, B, or C with cirrhosis: avoid use
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- cirrhosis
- caution: hepatic impairment, Child-Pugh Class B-C
Drug Interactions .
Overview
mitapivat
pyruvate kinase inhibitor
- CYP3A4 substrate
- P-gp inhibitor, weak
- CYP2B6 inducer, weak
- CYP2C8 inducer, weak
- CYP2C9 inducer, weak
- CYP2C19 inducer, weak
- CYP3A4 inducer, moderate
- UGT1A1 inducer
Contraindicated
- colchicine
- lonafarnib
- mavacamten
- ranolazine
- zoliflodacin
Avoid/Use Alternative
- abemaciclib
- acoramidis
- adagrasib
- alfentanil
- alpelisib
- apalutamide
- aprepitant
- artemether/lumefantrine
- atazanavir
- atogepant
- atrasentan
- avacopan
- avapritinib
- axitinib
- bedaquiline
- berotralstat
- bictegravir
- bosentan
- bosutinib
- brigatinib
- buprenorphine
- buspirone
- butalbital
- cabotegravir
- cabozantinib
- capivasertib
- capmatinib
- carbamazepine
- cariprazine
- cenobamate
- ceritinib
- chloramphenicol
- ciprofloxacin
- clarithromycin
- clofazimine
- cobicistat
- cobimetinib
- codeine
- conivaptan
- crizotinib
- cyclosporine
- dabigatran
- dabrafenib
- danazol
- daridorexant
- darolutamide
- darunavir
- defactinib
- deflazacort
- desogestrel (contraceptive)
- diazoxide
- dienogest (contraceptive)
- dihydrocodeine
- diltiazem
- dolutegravir
- doravirine
- dordaviprone
- doxorubicin
- dronedarone
- drospirenone (contraceptive)
- duvelisib
- efavirenz
- elacestrant
- elbasvir
- elexacaftor/tezacaftor/ivacaftor
- elinzanetant
- elvitegravir
- encorafenib
- ensartinib
- entrectinib
- enzalutamide
- erdafitinib
- erlotinib
- erythromycin
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- ethynodiol (contraceptive)
- etonogestrel (contraceptive)
- etravirine
- everolimus
- fedratinib
- felodipine
- fentanyl
- fexinidazole
- finerenone
- fluconazole
- fosamprenavir
- fosaprepitant
- fosphenytoin
- fostamatinib
- fruquintinib
- ganaxolone
- gepotidacin
- gilteritinib
- glasdegib
- glecaprevir
- grapefruit
- grazoprevir
- hydrocodone
- ibrexafungerp
- ibrutinib
- idelalisib
- imatinib
- irinotecan
- isavuconazonium
- isradipine
- istradefylline
- itraconazole
- ivacaftor
- ivosidenib
- ketoconazole
- larotrectinib
- lazertinib
- lefamulin
- lemborexant
- lenacapavir
- leniolisib
- letermovir
- levoketoconazole
- levonorgestrel (contraceptive)
- levonorgestrel (post-coital contraceptive)
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- lumateperone
- macitentan
- maraviroc
- medroxyprogesterone (contraceptive)
- meperidine
- methadone
- midazolam
- midostaurin
- mifepristone
- mitotane
- mobocertinib
- modafinil
- nafcillin
- naldemedine
- naloxegol
- nefazodone
- nelfinavir
- nerandomilast
- neratinib
- netupitant
- nevirapine
- nicardipine
- nifedipine
- nilotinib
- nirmatrelvir
- nirogacestat
- nisoldipine
- norelgestromin (contraceptive)
- norethindrone (contraceptive)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- olaparib
- oliceridine
- olutasidenib
- omaveloxolone
- oxycodone
- pacritinib
- palbociclib
- palovarotene
- pemigatinib
- pentobarbital
- pexidartinib
- phenobarbital
- phenytoin
- pimavanserin
- pirtobrutinib
- ponatinib
- posaconazole
- pralsetinib
- praziquantel
- pretomanid
- primidone
- quizartinib
- relugolix
- remibrutinib
- repotrectinib
- revumenib
- ribociclib
- rifabutin
- rifampin
- rifapentine
- rilpivirine
- rilzabrutinib
- rimegepant
- ripretinib
- ritonavir
- rivaroxaban
- roflumilast
- rolapitant
- sacituzumab govitecan
- samidorphan
- sebetralstat
- segesterone (contraceptive)
- selpercatinib
- selumetinib
- sevabertinib
- simvastatin
- sirolimus albumin-bound
- sonidegib
- sotorasib
- St. John's wort
- sufentanil
- sunvozertinib
- suzetrigine
- tadalafil
- taletrectinib
- tamoxifen
- tasimelteon
- tazemetostat
- tezacaftor/ivacaftor
- thiotepa
- ticagrelor
- tipranavir
- tofacitinib
- tolvaptan
- topotecan
- toremifene
- tramadol
- tucatinib
- ulipristal (post-coital contraceptive)
- valbenazine
- vanzacaftor/tezacaftor/deutivacaftor
- velpatasvir
- venetoclax
- verapamil
- voclosporin
- vonoprazan
- voriconazole
- voxilaprevir
- zanubrutinib
- ziftomenib
- zuranolone
Monitor/Modify Tx
- abiraterone acetate
- acalabrutinib
- afatinib
- aficamten
- aminophylline
- amlodipine
- apixaban
- armodafinil
- atorvastatin
- avatrombopag
- belzutifan
- bexarotene
- brexpiprazole
- butorphanol
- calcitriol
- cholecalciferol (vitamin D3)
- clobazam
- clozapine
- crinecerfont
- cyclophosphamide
- danshen
- deferasirox
- dexamethasone
- dicloxacillin
- digoxin
- disopyramide
- doxercalciferol
- echinacea
- edoxaban
- elafibranor
- elagolix
- enasidenib
- enfortumab vedotin
- eslicarbazepine acetate
- ethosuximide
- felbamate
- fludrocortisone
- garlic
- ginkgo
- ginseng, Asian
- glycerol phenylbutyrate
- griseofulvin
- guanfacine
- haloperidol
- hydrocortisone
- ifosfamide
- imipramine
- lapatinib
- levothyroxine
- liothyronine
- lurasidone
- macimorelin
- mavorixafor
- meropenem
- mirtazapine
- morphine
- nimodipine
- nortriptyline
- odevixibat
- oxcarbazepine
- paltusotine
- perampanel
- pioglitazone
- prednisone
- quetiapine
- quinidine (antiarrhythmic)
- repaglinide
- rufinamide
- sarilumab
- sildenafil
- sirolimus
- stiripentol
- tacrolimus
- talazoparib
- tecovirimat
- telotristat ethyl
- temsirolimus
- tenofovir alafenamide
- tenofovir disoproxil
- theophylline
- thyroid
- tiagabine
- tocilizumab
- topiramate
- tovorafenib
- ubrogepant
- vaborbactam
- vamorolone
- vemurafenib
- vilazodone
- vinblastine
- vorasidenib
- vortioxetine
- warfarin
- zonisamide
Caution Advised
- albendazole
- aliskiren
- alprazolam
- amiodarone
- apremilast
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- aripiprazole oral
- avanafil
- bazedoxifene
- belumosudil
- betamethasone
- bortezomib
- budesonide
- bupropion
- cannabis
- carisoprodol
- clindamycin
- copanlisib
- cortisone
- dapsone
- dasatinib
- diazepam
- drospirenone (hormone replacement)
- eliglustat
- esomeprazole
- eszopiclone
- ethinyl estradiol (hormone replacement)
- etoposide
- etrasimod
- exemestane
- fenfluramine
- fesoterodine
- finasteride
- flibanserin
- fostemsavir
- futibatinib
- gefitinib
- gepirone
- glyburide
- imlunestrant
- isotretinoin
- ivabradine
- ixabepilone
- ixazomib
- levonorgestrel (hormone replacement)
- levonorgestrel intrauterine device (contraceptive)
- lovastatin
- maribavir
- mefloquine
- methylprednisolone
- metoclopramide
- moxifloxacin
- nintedanib
- norethindrone (hormone replacement)
- omeprazole
- ondansetron
- osimertinib
- paclitaxel
- pazopanib
- pibrentasvir
- pitolisant
- polatuzumab vedotin
- prednisolone
- progesterone (hormone replacement)
- progesterone vaginal (hormone replacement)
- propafenone
- quinidine (CYP2D6 inhibitor)
- quinine
- raltegravir
- ramelteon
- regorafenib
- risperidone
- ritlecitinib
- ruxolitinib
- siponimod
- sorafenib
- sunitinib
- suvorexant
- telisotuzumab vedotin
- terbinafine
- tivozanib
- trabectedin
- trazodone
- tretinoin
- triamcinolone
- triazolam
- upadacitinib
- vandetanib
- vincristine
- vinorelbine
- vorapaxar
- zaleplon
- zolpidem
- zongertinib
Adverse Reactions .
Serious Reactions
- hepatocellular injury
- jaundice
- arrhythmia
Common Reactions
- headache
- insomnia
- testosterone incr. (male patients)
- estradiol decr. (male patients)
Safety/Monitoring .
Monitoring Parameters
LFTs, including ALT, AST, alk phos, and total bilirubin with fractionation, at baseline and q4wk x24wk, then as clinically indicated
Pregnancy/Lactation .
Pregnancy
Clinical Summary
benefits outweigh risks during pregnancy; inadequate human data available; no known risk of teratogenicity or embryo-fetal toxicity based on animal data at up to 13x MRHD, though risk of teratogenicity and embryo-fetal death based on animal data at 63x MRHD
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: for mitapivat: liver extensively; CYP450: 3A4 substrate
Excretion: for mitapivat: urine 49.6% (2.6% unchanged), feces 39.6% (<1% unchanged); Half-life: 3-5h
Subclass: Pyruvate Kinase Activators
Mechanism of Action
for mitapivat: binds pyruvate kinase tetramer, increasing pyruvate kinase activity, improving RBC lifespan and reducing hemolysis
Formulary .
No Formulary Selected
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