enzalutamide (Xtandi)
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Indications
- late-stage, castration-resistant prostate cancer previously treated with docetaxel
- progression of metastatic prostate cancer despite androgen-deprivation therapy[2]
- metastatic castration-resistant prostate cancer[1][2][3]
- prior to indication for chemotherapy (NGC, NICE)
- nonmetastatic castration-resistant prostate cancer[4]
- alternative to active surveillance alone in patients with low-risk or intermediate-risk localized prostate cancer[5]
Dosage
- 160 mg PO
Capsule: 40 mg, Tablets: 40 mg, 80 mg
Dosage adjustment in renal failure
* no dosage adjustment for hepatic impairment mild-to-severe (Child Pugh A to C)
Pharmacokinetics
- peak plasma time: 1 hr
- peak plasma concentration (steady-state):
- steady-state achieved by Day 28
Adverse effects
- fatigue
- hot flush
- back pain
- joint pain
- tissue swelling
- musculoskeletal pain
- headache
- paresthesia
- diarrhea
- upper respiratory infections
- lower respiratory infections
- dizziness
- spinal cord compression & cauda equina syndrome
- muscular weakness
- difficulty sleeping
- hematuria
- anxiety
- hypertension
- seizures (1%)
Drug interactions
- avoid use with CYP2C8 inhibitors
- if coadministration unavoidable, reduce enzalutamide dose to 80 mg QD
- avoid use with CYP3A4 inducers
- if coadministration unavoidable, increase enzalutamide dose to 240 mg QD
- also see Medscape: enzalutamide (Rx)[6]
Mechanism of action
More general terms
References
- ↑ Jump up to: 1.0 1.1 FDA News Release: Aug. 31, 2012 FDA approves new treatment for a type of late stage prostate cancer http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm317838.htm
- ↑ Jump up to: 2.0 2.1 2.2 Beer TM et al Enzalutamide in Metastatic Prostate Cancer before Chemotherapy. N Engl J Med. June 1, 2014 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24881730 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1405095
- ↑ Jump up to: 3.0 3.1 Rathkopf DE, Beer TM, Loriot Y et al Radiographic Progression-Free Survival as a Clinically Meaningful End Point in Metastatic Castration-Resistant Prostate Cancer. The PREVAIL Randomized Clinical Trial. JAMA Oncol. Published online March 8, 2018 PMID: https://www.ncbi.nlm.nih.gov/pubmed/29522174 https://jamanetwork.com/journals/jamaoncology/fullarticle/2674383
- ↑ Jump up to: 4.0 4.1 Hussain M, Fizazi K, Saad F et al. Enzalutamide in men with nonmetastatic, castration-resistant prostate cancer. N Engl J Med 2018 Jun 28; 378:2465. PMID: https://www.ncbi.nlm.nih.gov/pubmed/29949494 https://www.nejm.org/doi/10.1056/NEJMoa1800536
Smith MR. Progress in nonmetastatic prostate cancer. N Engl J Med 2018 Jun 28; 378:2531 PMID: https://www.ncbi.nlm.nih.gov/pubmed/29949488 https://www.nejm.org/doi/10.1056/NEJMe1805733 - ↑ Jump up to: 5.0 5.1 Bassett M Xtandi During AS Reduced Progression Risk in Early Prostate Cancer. Risk of disease progression cut by 46% versus those on active surveillance alone. MedPage Today June 16, 2022 https://www.medpagetoday.com/hematologyoncology/prostatecancer/99291
Shore ND, Renzulli J, Fleshner E et al Active Surveillance Plus Enzalutamide Monotherapy vs Active Surveillance Alone in Patients With Low-risk or Intermediate-risk Localized Prostate Cancer. The ENACT Randomized Clinical Trial. JAMA Oncol. Published online June 16, 2022 PMID: https://www.ncbi.nlm.nih.gov/pubmed/35708696 https://jamanetwork.com/journals/jamaoncology/fullarticle/2793567 - ↑ Jump up to: 6.0 6.1 Medscape: enzalutamide (Rx) https://reference.medscape.com/drug/xtandi-enzalutamide-999769