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Lynkuet
elinzanetant
Adult Dosing .
Dosage forms: CAP: 60 mg
vasomotor symptoms, moderate-severe menopausal
- [120 mg PO qhs]
- Info: D/C if ALT or AST >5x ULN, or if ALT or AST >3x ULN and total bilirubin >2x ULN; do not open cap
renal dosing
- [see below]
- eGFR >15: no adjustment; eGFR <15: not defined
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B or C: avoid use
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- ALT or AST >2x ULN
- bilirubin >2x ULN
- hepatic impairment, Child-Pugh Class B-C
- pregnancy
- caution: patients of childbearing potential
- caution: seizure history
- caution: seizure threshold, lowered
Drug Interactions .
Overview
elinzanetant
NK-1/NK-3 antagonist
- CYP3A4 substrate
- CYP3A4 inhibitor, weak
- CNS depression
- lowers seizure threshold
Contraindicated
- cisapride
- eliglustat
Avoid/Use Alternative
- adagrasib
- aldesleukin
- alprazolam
- amifampridine
- apalutamide
- atazanavir
- bosentan
- butalbital
- carbamazepine
- cenobamate
- ceritinib
- chloramphenicol
- clarithromycin
- clonidine
- cobicistat
- codeine
- colchicine
- dabrafenib
- doxylamine
- efavirenz
- encorafenib
- enzalutamide
- ethanol
- etravirine
- fexinidazole
- fosphenytoin
- hydrocodone
- idelalisib
- iohexol
- isocarboxazid
- itraconazole
- ivosidenib
- kava
- ketoconazole
- kratom
- levoketoconazole
- lonafarnib
- lopinavir/ritonavir
- lorlatinib
- mavacamten
- meperidine
- metaxalone
- methadone
- metoclopramide
- midazolam
- mifepristone
- mitapivat
- mitotane
- modafinil
- nafcillin
- nefazodone
- nelfinavir
- oxybate
- oxycodone
- pacritinib
- pentobarbital
- pexidartinib
- phenelzine
- phenobarbital
- phenytoin
- pimozide
- posaconazole
- pralsetinib
- primidone
- promethazine
- propafenone
- repotrectinib
- ribociclib
- rifapentine
- ritonavir
- ropeginterferon alfa-2b
- simvastatin
- sotorasib
- thalidomide
- tipranavir
- tranylcypromine
- trimethobenzamide
- tucatinib
- voriconazole
- zuranolone
Monitor/Modify Tx
- abemaciclib
- acalabrutinib
- alfentanil
- amiodarone
- aprepitant
- avacopan
- avanafil
- avapritinib
- baclofen intrathecal
- berotralstat
- brigatinib
- buprenorphine
- bupropion
- butorphanol
- capivasertib
- chlordiazepoxide
- chlorpromazine
- ciprofloxacin
- clobazam
- clofazimine
- clonazepam
- clorazepate
- clozapine
- conivaptan
- crizotinib
- cyclosporine
- danazol
- daridorexant
- darunavir
- desflurane
- dexmedetomidine
- dexmedetomidine injection
- diazepam
- dihydrocodeine
- diltiazem
- disopyramide
- docetaxel
- dofetilide
- domperidone
- dronedarone
- droperidol
- duvelisib
- entrectinib
- erythromycin
- esketamine
- estazolam
- eszopiclone
- ethanol (in some formulations)
- etomidate
- everolimus
- fedratinib
- felodipine
- fentanyl
- finerenone
- flibanserin
- fluconazole
- fluphenazine
- flurazepam
- fosamprenavir
- gabapentin
- gabapentin enacarbil
- gepirone
- grapefruit
- hydromorphone
- hydroxyzine
- ibrutinib
- ifosfamide
- imatinib
- iopamidol
- isavuconazonium
- isoflurane
- ivabradine
- ixabepilone
- ketamine
- lefamulin
- lemborexant
- lenacapavir
- letermovir
- levorphanol
- lomitapide
- lorazepam
- lovastatin
- lumateperone
- lurasidone
- lurbinectedin
- methohexital
- mirtazapine
- mobocertinib
- morphine
- nalbuphine
- nelarabine
- netupitant
- nifedipine
- nilotinib
- nimodipine
- nirogacestat
- nisoldipine
- olanzapine
- oliceridine
- opicapone
- opium
- oxazepam
- oxybutynin
- oxymorphone
- pemigatinib
- pentazocine
- perphenazine
- pregabalin
- propofol
- quazepam
- quinidine (antiarrhythmic)
- red yeast rice
- remifentanil
- remimazolam
- rilzabrutinib
- selpercatinib
- selumetinib
- sevoflurane
- sirolimus
- sirolimus albumin-bound
- sufentanil
- suvorexant
- tacrolimus
- tadalafil
- taletrectinib
- tapentadol
- temazepam
- temsirolimus
- thioridazine
- thiothixene
- tolvaptan
- tramadol
- triazolam
- ubrogepant
- vardenafil
- venetoclax
- verapamil
- vinblastine
- vincristine
- vinorelbine
- warfarin
- zaleplon
- zanubrutinib
- ziconotide
- zolpidem
Caution Advised
- 5-HTP
- acetazolamide
- allopurinol
- almotriptan
- amantadine
- amitriptyline
- amlodipine
- amoxapine
- apomorphine
- apraclonidine ophthalmic
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- aripiprazole oral
- asciminib
- asenapine
- atorvastatin
- baclofen
- belumosudil
- berberine
- bicalutamide
- brexpiprazole
- brimonidine ophthalmic
- brimonidine topical
- brivaracetam
- bromocriptine
- brompheniramine
- buspirone
- busulfan
- cannabidiol
- cannabis
- carbinoxamine
- cariprazine
- carisoprodol
- cetirizine
- chamomile, German
- chlophedianol
- chlorambucil
- chlorpheniramine
- chlorzoxazone
- cilostazol
- cimetidine
- citalopram
- clemastine
- clomipramine
- clotrimazole oropharyngeal
- cobimetinib
- cranberry
- cyclobenzaprine
- cyclophosphamide
- cyproheptadine
- dantrolene
- darifenacin
- desipramine
- desvenlafaxine
- deutetrabenazine
- dexbrompheniramine
- dexchlorpheniramine
- dichlorphenamide
- difelikefalin
- difenoxin
- dihydroergotamine
- dimenhydrinate
- diosmin
- diphenhydramine
- diphenoxylate
- doxepin
- doxepin topical
- dronabinol
- duloxetine
- eletriptan
- entacapone
- eplerenone
- ergotamine
- escitalopram
- eslicarbazepine acetate
- ethinyl estradiol (contraceptive)
- ethosuximide
- felbamate
- fenfluramine
- fesoterodine
- fluoxetine
- fluvoxamine
- fosaprepitant
- foslevodopa
- fostamatinib
- frovatriptan
- ganaxolone
- gepotidacin
- ginkgo
- givinostat
- givosiran
- glecaprevir
- glofitamab
- glycopyrrolate
- goldenseal
- grazoprevir
- guanfacine
- haloperidol
- hydroxychloroquine
- hyoscyamine
- iloperidone
- imipramine
- isoniazid
- istradefylline
- ivacaftor
- lacosamide
- lamotrigine
- lapatinib
- larotrectinib
- lasmiditan
- lazertinib
- levetiracetam
- levocetirizine
- levodopa
- levomilnacipran
- linvoseltamab
- lofexidine
- loxapine
- lumacaftor/ivacaftor
- magnesium citrate
- maribavir
- mavorixafor
- meclizine
- melatonin
- meprobamate
- methocarbamol
- methsuximide
- methyldopa
- methylergonovine
- metyrapone
- metyrosine
- milnacipran
- molindone
- mosunetuzumab
- mycophenolate mofetil
- naltrexone
- naratriptan
- nicardipine
- nortriptyline
- orphenadrine
- osilodrostat
- oxcarbazepine
- palbociclib
- paliperidone
- palovarotene
- paroxetine
- passion flower
- pazopanib
- peppermint
- perampanel
- pheniramine
- pibrentasvir
- pirtobrutinib
- polyethylene glycol
- polyethylene glycol/electrolytes
- pramipexole
- procarbazine
- prochlorperazine
- protriptyline
- pyrilamine
- quercetin
- quetiapine
- ramelteon
- ranolazine
- rasagiline
- remdesivir
- resveratrol
- rifabutin
- rifampin
- risperidone
- ritlecitinib
- rizatriptan
- roflumilast
- roflumilast topical
- ropinirole
- rotigotine transdermal
- rucaparib
- rufinamide
- safinamide
- scopolamine
- selegiline
- selegiline transdermal
- selinexor
- sertraline
- sirolimus topical
- sodium picosulfate
- solifenacin
- spironolactone
- St. John's wort
- stiripentol
- sulfate bowel prep
- sumatriptan
- tasimelteon
- tetrabenazine
- thiotepa
- tiagabine
- ticagrelor
- tizanidine
- tolcapone
- tolterodine
- topiramate
- trazodone
- treosulfan
- trifluoperazine
- trihexyphenidyl
- trimipramine
- triprolidine
- trofinetide
- trospium
- valbenazine
- valerian
- valproic acid
- venlafaxine
- vigabatrin
- vilazodone
- viloxazine
- vonoprazan
- xanomeline
- zileuton
- ziprasidone
- zolmitriptan
- zonisamide
Adverse Reactions .
Serious Reactions
- CNS depression
- impaired mental alertness, next-day
- hepatotoxicity
- seizures
Common Reactions
- headache
- fatigue
- dizziness
- somnolence
- abdominal pain
- rash
- diarrhea
- muscle spasm
- GERD
- nausea
- photosensitivity
Safety/Monitoring .
Monitoring Parameters
pregnancy test before tx start and if pregnancy suspected during tx; LFTs (incl. alk phos, ALT/AST, total and direct bilirubin) at baseline, then ALT/AST 3mo after tx start
Pregnancy/Lactation .
Pregnancy
Clinical Summary
contraindicated during pregnancy; no human data available; no known risk of teratogenicity, though risk of stillbirth based on animal data at 1x systemic exposure and risk of embryo loss and decr. fetal wt at 16x systemic exposure
Individuals of Reproductive Potential
obtain pregnancy test before tx start and if pregnancy suspected during tx; avoid pregnancy by using effective contraception during tx and x2wk after D/C in patients of childbearing potential
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: liver; CYP450: 3A4 substrate; Info: active metabolites
Excretion: feces 90% (50% unchanged), urine <1%; Half-life: 45h
Subclass: Neurokinin Receptor Antagonists, Gynecologic
Mechanism of Action
antagonizes neurokinin 1 and 3 receptors on kisspeptin/neurokinin B/dynorphin (KNDy) neurons, modulating neuronal activity involved in thermoregulation
Formulary .
No Formulary Selected
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