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Truqap
capivasertib
Adult Dosing .
Dosage forms: TAB: 160 mg, 200 mg
Special Note
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing incl. toxicity-related dose adjustments
hormone receptor-positive HER2-negative breast CA, locally advanced or metastatic
- [400 mg PO bid on days 1-4 of 7-day cycle]
- Info: for pts w/ PIK3CA/AKT1/PTEN alteration w/ dz progression on endocrine-based tx; use w/ fulvestrant; give w/ LHRH agonist in pre/perimenopausal female pts; consider giving w/ LHRH agonist in male pts; do not cut/crush/chew tab
renal dosing
- [see below]
- CrCl >30: no adjustment; CrCl <30: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- bilirubin 1.1-1.5x ULN or AST >ULN: no adjustment; bilirubin >1.5x ULN: not defined, caution advised
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- avoid: breastfeeding
- caution: female pts of reproductive potential
- caution: male pts of reproductive potential
- caution: bilirubin >1.5x ULN
- caution: diabetes mellitus
- caution: hyperglycemia risk
Drug Interactions .
Overview
capivasertib
kinase inhibitor
- CYP3A4 substrate
- CYP2D6 inhibitor, moderate
- CYP3A4 inhibitor, weak
- UGT1A1 inhibitor
- hyperglycemic effects
Contraindicated
- cisapride
- eliglustat
- thioridazine
Avoid/Use Alternative
- adagrasib
- alprazolam
- apalutamide
- atazanavir
- belinostat
- bosentan
- butalbital
- carbamazepine
- cenobamate
- ceritinib
- chloramphenicol
- clarithromycin
- cobicistat
- codeine
- colchicine
- dabrafenib
- dihydrocodeine
- doxorubicin
- efavirenz
- encorafenib
- enzalutamide
- etravirine
- fexinidazole
- fosamprenavir
- fosphenytoin
- grapefruit
- hydrocodone
- idelalisib
- irinotecan
- itraconazole
- ivosidenib
- ketoconazole
- lenacapavir
- levoketoconazole
- lisdexamfetamine
- lonafarnib
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- mavacamten
- meperidine
- methadone
- mifepristone
- mitapivat
- mitotane
- modafinil
- nafcillin
- nefazodone
- nelfinavir
- oliceridine
- oxycodone
- pacritinib
- pentobarbital
- pexidartinib
- phenobarbital
- phenytoin
- pimozide
- pirfenidone
- posaconazole
- pralsetinib
- primidone
- propafenone
- repotrectinib
- ribociclib
- rifabutin
- rifampin
- rifapentine
- ritonavir
- sacituzumab govitecan
- simvastatin
- sotorasib
- St. John's wort
- tamsulosin
- tipranavir
- tramadol
- tucatinib
- voriconazole
Monitor/Modify Tx
- abemaciclib
- acalabrutinib
- acarbose
- acetaminophen
- alfentanil
- alogliptin
- amiodarone
- amlodipine
- aprepitant
- aripiprazole bimonthly injection
- aripiprazole oral
- asciminib
- atorvastatin
- avacopan
- avanafil
- avapritinib
- belumosudil
- berberine
- berotralstat
- bexagliflozin
- bicalutamide
- brexpiprazole
- brigatinib
- bromocriptine
- canagliflozin
- chlorzoxazone
- cilostazol
- cimetidine
- ciprofloxacin
- clofazimine
- clotrimazole oropharyngeal
- clozapine
- colesevelam
- conivaptan
- cranberry
- crizotinib
- cyclosporine
- danazol
- dapagliflozin
- daridorexant
- darunavir
- desipramine
- deutetrabenazine
- dextroamphetamine
- diltiazem
- diosmin
- disopyramide
- docetaxel
- dofetilide
- domperidone
- dronedarone
- dulaglutide
- duvelisib
- empagliflozin
- entrectinib
- ertugliflozin
- erythromycin
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- everolimus
- exenatide
- fedratinib
- felodipine
- fentanyl
- finerenone
- flecainide
- flibanserin
- fluconazole
- fluvoxamine
- fosaprepitant
- fostamatinib
- gepirone
- ginkgo
- givinostat
- givosiran
- glecaprevir
- glimepiride
- glipizide
- glyburide
- goldenseal
- grazoprevir
- ibrutinib
- iloperidone
- imatinib
- imipramine
- infigratinib
- insulin
- isavuconazonium
- isoniazid
- istradefylline
- ivabradine
- ivacaftor
- ixabepilone
- kratom
- lapatinib
- larotrectinib
- lazertinib
- lefamulin
- lemborexant
- letermovir
- linagliptin
- liraglutide
- lomitapide
- lovastatin
- lumateperone
- lurasidone
- lurbinectedin
- maribavir
- mavorixafor
- metformin
- metoprolol
- midazolam
- miglitol
- mobocertinib
- nateglinide
- nebivolol
- netupitant
- nicardipine
- nifedipine
- nilotinib
- nimodipine
- nirogacestat
- nisoldipine
- nortriptyline
- osilodrostat
- palbociclib
- pazopanib
- pemigatinib
- peppermint
- perphenazine
- pibrentasvir
- pioglitazone
- pirtobrutinib
- pitolisant
- pramlintide
- propranolol
- quercetin
- quinidine (antiarrhythmic)
- ranolazine
- red yeast rice
- remdesivir
- repaglinide
- resveratrol
- ritlecitinib
- rosiglitazone
- rucaparib
- saxagliptin
- selpercatinib
- selumetinib
- semaglutide
- sirolimus
- sirolimus albumin-bound
- sitagliptin
- spironolactone
- stiripentol
- sufentanil
- tacrolimus
- tadalafil
- temsirolimus
- tetrabenazine
- ticagrelor
- tirzepatide
- tolvaptan
- treosulfan
- triazolam
- trofinetide
- ubrogepant
- vardenafil
- venetoclax
- verapamil
- viloxazine
- vinblastine
- vincristine
- vinorelbine
- vonoprazan
- voxelotor
- warfarin
- xanomeline
- yohimbe
- zanubrutinib
- zileuton
Caution Advised
- armodafinil
- artemether/lumefantrine
- belzutifan
- bexarotene
- bictegravir
- cariprazine
- clobazam
- cobimetinib
- cyclophosphamide
- danshen
- darolutamide
- dexamethasone
- dicloxacillin
- dihydroergotamine
- echinacea
- elafibranor
- elagolix
- enasidenib
- eplerenone
- ergotamine
- eslicarbazepine acetate
- felbamate
- garlic
- ginseng, Asian
- glycerol phenylbutyrate
- griseofulvin
- meropenem
- methylergonovine
- nevirapine
- olutasidenib
- omaveloxolone
- oxcarbazepine
- palovarotene
- perampanel
- prednisone
- roflumilast
- roflumilast topical
- rufinamide
- sarilumab
- sirolimus topical
- somatropin
- suzetrigine
- tamoxifen
- tazemetostat
- tecovirimat
- telotristat ethyl
- tocilizumab
- topiramate
- tovorafenib
- vaborbactam
- vamorolone
- vemurafenib
- vorasidenib
- vortioxetine
Adverse Reactions .
Serious Reactions
- hyperglycemia, severe
- ketoacidosis
- diarrhea, severe
- dehydration
- erythema multiforme
- hand-foot syndrome
- drug rxn w/ eosinophilia and systemic sx
- acute kidney injury
Common Reactions
- diarrhea
- skin rxn
- fatigue
- nausea
- stomatitis
- vomiting
- hyperglycemia
- appetite decr.
- headache
- UTI
- acute kidney injury
- glucose incr.
- lymphocytes decr.
- Hgb decr.
- neutrophils decr.
- Plt decr.
- triglycerides incr.
- ALT incr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; HbA1C at baseline, then q3mo, and as clinically indicated; fasting glucose at baseline, then on day 3 or 4 of 7-day cycle on wk 1, 2, 4, 6, 8, then qmo, and as clinically indicated
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; risk of embryo-fetal toxicity, incl. decr. fetal weight and embryo-fetal death based on animal data at 0.7x systemic exposure and drug's mechanism of action
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective contraception during tx and x1mo after D/C in female pts and during tx and x4mo after D/C in male pts
Lactation
Clinical Summary
avoid breastfeeding; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: unknown; CYP450: 3A4 substrate; UGT: 2B7 substrate
Excretion: feces 50%, urine 45%; Half-life: 8.3h
Subclass: Kinase Inhibitors, AKT Inhibitors
Mechanism of Action
competitively inhibits all three AKT isoforms (AKT1/2/3), resulting in reduced tumor growth
Formulary .
No Formulary Selected
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