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Abemaciclib (Monograph)

Brand name: Verzenio
Drug class: Antineoplastic Agents

Medically reviewed by Drugs.com on Aug 24, 2023. Written by ASHP.

Introduction

Antineoplastic agent; a selective inhibitor of cyclin-dependent kinases 4 (CDK4) and 6 (CDK6).1 2 3

Uses for Abemaciclib

Breast Cancer

In combination with an aromatase inhibitor or tamoxifen for the adjuvant treatment of hormone receptor-positive, human epidermal growth factor receptor type 2 (HER2)-negative, node-positive, early-stage breast cancer in adults who are at high risk for recurrence.1

In combination with an aromatase inhibitor (e.g., anastrozole, letrozole) for initial treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer in men and postmenopausal women.1 14 18

In combination with fulvestrant for treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer in adults with disease progression following endocrine therapy.1 2 19 22

Monotherapy for treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer in adults with disease progression following endocrine therapy and prior chemotherapy for metastatic disease.1 3

Abemaciclib Dosage and Administration

General

Pretreatment Screening

Patient Monitoring

Dispensing and Administration Precautions

Other General Considerations

Administration

Oral Administration

Administer orally twice daily without regard to food at approximately the same time each day.1

Swallow tablets whole; do not break, chew, crush, or split.1

If a dose is missed or vomited, take the next dose at the regularly scheduled time.1 Do not double the dose or take extra doses.1

Dosage

Adults

Breast Cancer
Adjuvant Therapy for Early-stage Breast Cancer
Oral

150 mg twice daily in combination with an aromatase inhibitor (e.g., anastrozole, letrozole) or tamoxifen.1 Continue therapy for 2 years or until disease progression or unacceptable toxicity occurs.1

Treat premenopausal or perimenopausal women receiving combination therapy with abemaciclib and an aromatase inhibitor or fulvestrant with a gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone) agonist (e.g., goserelin) according to current standards of care.1

Treat men receiving combination therapy with abemaciclib and an aromatase inhibitor with a GnRH agonist according to current standards of care.1

Initial Therapy for Advanced Breast Cancer
Oral

150 mg twice daily in combination with an aromatase inhibitor (e.g., anastrozole, letrozole).1 Continue therapy until disease progression or unacceptable toxicity occurs.1

Treat premenopausal or perimenopausal women receiving combination therapy with abemaciclib and aromatase inhibitor with a gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone) agonist (e.g., goserelin) according to current standards of care.1

Treat men receiving combination therapy with abemaciclib and an aromatase inhibitor with a GnRH agonist according to current standards of care.1

Previously Treated Advanced Breast Cancer: Combination Therapy
Oral

150 mg twice daily given continuously; administer in combination with fulvestrant 500 mg IM on days 1, 15, and 29 of cycle 1 followed by once monthly thereafter.1

Treat premenopausal or perimenopausal women receiving combination therapy with abemaciclib and fulvestrant with a gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone) agonist (e.g., goserelin) according to current standards of care.1

Previously Treated Advanced Breast Cancer: Monotherapy
Oral

200 mg twice daily.1

Continue therapy until disease progression or unacceptable toxicity occurs.1

Dosage Modification for Toxicity
Oral

Adverse effects may require temporary interruption and/or dosage reduction or discontinuance.1

Dosages <50 mg twice daily not recommended; discontinue drug if 50-mg twice daily dosage is not tolerated.1

Recommended dosage modifications for abemaciclib during monotherapy or combination therapy with fulvestrant or an aromatase inhibitor in Table 1.1

Table 1: Dosage Modifications for Abemaciclib Toxicity

Dosage Modification after Recovery from Toxicity

Dosage Modification after Recovery from Toxicity

Toxicity Occurrence

Single-agent Abemaciclib (Starting Dosage = 200 mg twice daily)

Abemaciclib in Combination with Fulvestrant, Tamoxifen, or an Aromatase Inhibitor (Starting Dosage = 150 mg twice daily)

First

Restart at 150 mg twice daily

Restart at 100 mg twice daily

Second

Restart at 100 mg twice daily

Restart at 50 mg twice daily

Third

Restart at 50 mg twice daily

Discontinue abemaciclib

Fourth

Discontinue abemaciclib

Hematologic Toxicity
Oral

If grade 4 hematologic toxicity occurs, temporarily interrupt abemaciclib therapy.1 When toxicity improves to grade 2 or less, resume therapy at reduced dosage.1

For first occurrence of grade 3 hematologic toxicity, temporarily interrupt abemaciclib therapy.1 When toxicity improves to grade 2 or less, resume therapy at same dosage.1 If grade 3 hematologic toxicity recurs, temporarily interrupt abemaciclib therapy; upon improvement to grade 2 or less, resume therapy at reduced dosage.1

If grade 1 or 2 hematologic toxicity occurs, no dosage modification required.1

May administer hematopoietic growth factors (e.g., granulocyte colony-stimulating factor [G-CSF]) if clinically indicated; however, withhold abemaciclib for ≥48 hours after the last dose of a hematopoietic growth factor and until the toxicity improves to grade 2 or less.1

Diarrhea
Oral

If grade 3 or 4 diarrhea or diarrhea requiring hospitalization occurs, temporarily interrupt abemaciclib therapy.1 When diarrhea improves to grade 1 or less, resume therapy at reduced dosage.1

For persistent grade 2 diarrhea lasting ≥24 hours, temporarily interrupt abemaciclib therapy.1 When diarrhea resolves, resume therapy at same dosage.1 If grade 2 diarrhea persists or recurs despite optimal supportive measures, temporarily interrupt abemaciclib therapy; upon improvement to grade 1 or less, resume therapy at reduced dosage.1

If grade 1 diarrhea occurs, no dosage modification required.1

Hepatic Toxicity
Oral

If grade 4 serum ALT and/or AST elevations (i.e., >20 times the ULN) or serum ALT and/or AST elevations >3 times the ULN with total bilirubin concentrations >2 times the ULN in the absence of cholestasis occur, discontinue abemaciclib therapy.1

If grade 3 serum ALT and/or AST elevations (i.e., >5 times the ULN, but ≤20 times the ULN) with total bilirubin concentrations ≤2 times the ULN occur, temporarily interrupt abemaciclib therapy.1 When toxicity improves to grade 1 or less, resume therapy at reduced dosage.1

If grade 2 serum ALT and/or AST elevations (i.e., >3 times the ULN, but ≤5 times the ULN) with total bilirubin concentrations ≤2 times the ULN occur, no dosage modification required.1 For persistent or recurrent grade 2 serum ALT and/or AST elevations with total bilirubin concentrations ≤2 times the ULN, temporarily interrupt abemaciclib therapy; upon improvement to grade 1 or baseline, resume therapy at reduced dosage.1

If grade 1 serum ALT and/or AST elevations (i.e., exceeding the ULN, but ≤3 times the ULN) with total bilirubin concentrations ≤2 times the ULN occur, no dosage modification required.1

Interstitial Lung Disease (ILD)/Pneumonitis
Oral

If grade 3 or 4 ILD/pneumonitis occurs, permanently discontinue abemaciclib therapy.1 17

If grade 2 ILD/pneumonitis occurs, no dosage modification required.1 If grade 2 ILD/pneumonitis persists or recurs despite optimal supportive measures for up to 7 days, temporarily interrupt abemaciclib therapy; upon improvement to grade 1 or baseline, resume therapy at reduced dosage.1

If grade 1 ILD/pneumonitis occurs, no dosage modification required.1

Venous Thromboembolic Event
Oral

For venous thromboembolic events of any grade in patients with early-stage breast cancer, interrupt abemaciclib therapy and treat as clinically indicated.1 When the patient is clinically stable, resume abemaciclib therapy.1

For grade 1 or 2 venous thromboembolic events in patients with advanced or metastatic breast cancer, no dosage adjustment is necessary.1

For grade 3 or 4 venous thromboembolic events in patients with advanced or metastatic breast cancer, interrupt abemaciclib therapy and treat as clinically indicated.1 When the patient is clinically stable, resume abemaciclib therapy.1

Other Toxicity
Oral

If grade 3 or 4 adverse reactions occur, temporarily interrupt abemaciclib therapy.1 When toxicity improves to grade 1 or baseline, resume therapy at reduced dosage.1

If grade 2 adverse reactions occur, no dosage modification required.1 If grade 2 adverse reactions persist or recur despite optimal supportive measures for up to 7 days, temporarily interrupt abemaciclib therapy; upon improvement to grade 1 or baseline, resume therapy at reduced dosage.1

If grade 1 adverse reactions occur, no dosage modification required.1

Dosage Modification with Concomitant Drugs or Foods Affecting Hepatic Microsomal Enzymes
Oral

Avoid concomitant use with ketoconazole.1

If used concomitantly with other potent CYP3A inhibitors, reduce initial abemaciclib dosage (200 or 150 mg twice daily depending on indication) to 100 mg twice daily or, in those already receiving a reduced dosage of abemaciclib (100 mg twice daily), reduce dosage of abemaciclib to 50 mg twice daily.1

If used concomitantly with moderate CYP3A inhibitors, monitor for signs of abemaciclib toxicity and consider dosage modification for adverse reactions (see Table 1).1

Prescribing Limits

Adults

Breast Cancer
Oral

Dosages <50 mg twice daily not recommended.1

Special Populations

Hepatic Impairment

Severe preexisting hepatic impairment (Child-Pugh class C): Reduce dosage frequency to once daily.1

Mild or moderate preexisting hepatic impairment (Child-Pugh class A or B): No dosage adjustment required.1

Renal Impairment

Mild or moderate renal impairment (Clcr 30–89 mL/minute): No dosage adjustment required.1

Severe renal impairment (Clcr <30 mL/minute), end-stage renal disease, or patients receiving dialysis: No specific dosage recommendations at this time.1

Geriatric Patients

No specific dosage recommendations at this time.1

Cautions for Abemaciclib

Contraindications

Warnings/Precautions

Diarrhea

Diarrhea occurs frequently.1 May result in dehydration or infection.1 Median time to onset: 6–8 days.1 Median duration of grade 2 or 3 diarrhea: 6–11 or 5–8 days, respectively, in clinical trials.1

Monitor for development of diarrhea and immediately treat as necessary with appropriate therapy (e.g., antidiarrheal agents, fluid replacement) at first sign of loose stools.1 If diarrhea occurs, temporary interruption, dosage reduction, or discontinuance of abemaciclib may be necessary.1

Neutropenia

Neutropenia, including febrile neutropenia and neutropenic sepsis, reported.1 Median time to onset of grade 3 or greater neutropenia: 29–33 days.1 Median duration of grade 3 or greater neutropenia: 11–16 days.1

Monitor CBC at baseline, every 2 weeks during the initial 2 months of therapy, monthly during the next 2 months, and then as clinically indicated.1 If neutropenia occurs, temporary interruption, dosage reduction, or discontinuance of abemaciclib may be necessary.1 May administer hematopoietic growth factors (e.g., G-CSF) if clinically indicated; however, withhold abemaciclib for ≥48 hours after the last dose of hematopoietic growth factor and until the toxicity improves to grade 2 or less.1

ILD/Pneumonitis

Severe, life-threatening, or fatal ILD/pneumonitis reported with CDK4 and CDK6 inhibitors, including abemaciclib.1

Monitor patients clinically and by radiographic imaging for manifestations of ILD or pneumonitis.1

If manifestations of ILD or pneumonitis occur and other etiologies (e.g., infection, neoplastic) have been excluded, temporary interruption, dosage reduction, or discontinuance of abemaciclib may be necessary.1 17

Hepatic Toxicity

Hepatotoxicity reported.1 Median time to onset of grade 3 or greater elevations in AST concentrations: 71–185 days; these elevations resolved in 11–15 days.1

Monitor liver function tests (i.e., serum ALT, AST, and bilirubin concentrations) at baseline, every 2 weeks during the initial 2 months of therapy, monthly during the next 2 months, and then as clinically indicated.1 If hepatotoxicity occurs, temporary interruption, dosage reduction, or discontinuance of abemaciclib may be necessary.1

Thromboembolic Events

Venous thromboembolic events (i.e., DVT, pulmonary embolism, pelvic venous thrombosis, cerebral venous sinus thrombosis, subclavian and axillary vein thrombosis, inferior vena cava thrombosis), sometimes fatal, reported.1

Monitor for manifestations of venous thromboembolic events, including pulmonary embolism.1 Interrupt abemaciclib therapy in patients with early-stage breast cancer who develop a venous thromboembolic event of any grade and in patients with advanced or metastatic breast cancer who develop a grade 3 or 4 venous thromboembolic event.1 Initiate appropriate medical intervention.1

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; embryofetal toxicity and teratogenicity demonstrated in animals.1

Avoid pregnancy during therapy.1 Females of reproductive potential should use effective contraceptive methods while receiving abemaciclib and for ≥3 weeks after the drug is discontinued.1 If used during pregnancy or patient becomes pregnant, apprise of potential fetal hazard.1

Specific Populations

Pregnancy

May cause fetal harm.1

In females of reproductive potential, manufacturer recommends a pregnancy test prior to initiating abemaciclib therapy.1

Lactation

Not known whether abemaciclib distributes into human milk or if drug has any effect on milk production or nursing infant.1 Discontinue nursing during therapy and for ≥3 weeks after drug is discontinued.1

Females and Males of Reproductive Potential

Animal studies suggest abemaciclib may impair male fertility.1

Pediatric Use

Safety and efficacy not established.1

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.1 Most common grade 3 or 4 toxicities included neutropenia, diarrhea, fatigue, nausea, dehydration, leukopenia, anemia, infection, and elevated serum ALT concentrations.1

Hepatic Impairment

Mild or moderate hepatic impairment did not substantially affect potency-adjusted total exposure to unbound drug and active metabolites; dosage adjustment not necessary.1

Severe hepatic impairment prolonged mean elimination half-life and increased potency-adjusted total exposure to unbound drug and active metabolites; dosage adjustment recommended.1

Renal Impairment

Mild or moderate renal impairment did not substantially affect systemic exposure of abemaciclib; dosage adjustment not necessary.1

Not studied in patients with severe renal impairment.1

Abemaciclib increases Scr by inhibiting tubular secretion of creatinine;1 does not cause clinically important change in GFR.1

Common Adverse Effects

Adverse effects reported in ≥20% of patients: Diarrhea, neutropenia, nausea, abdominal pain, infections, fatigue, anemia, leukopenia, decreased appetite, vomiting, headache, alopecia, thrombocytopenia.1

Drug Interactions

Metabolized mainly by CYP3A4 to active metabolites (M-2, M-18, and M-20).1

Autoinhibition of abemaciclib metabolism via CYP3A4 not observed.1

In vitro studies indicate inhibition of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) by abemaciclib.1 Abemaciclib, M-2, and M-20 inhibit organic cation transporter (OCT) 2, multidrug and toxic compound extrusion protein (MATE) 1, and MATE2K, but do not inhibit OCT1, organic anion transport protein (OATP) 1B1, OATP1B3, organic anion transporter (OAT) 1, and OAT3.1 In vitro, the drug is a substrate for P-gp and BCRP, but abemaciclib, M-2, and M-20 are not substrates for OCT1, OATP1B1, or OATP1B3.1

Drugs and Foods Affecting Hepatic Microsomal Enzymes

Potent or moderate CYP3A inhibitors: Possible increased systemic exposure to abemaciclib and its active metabolites and increased risk of adverse effects.1 Avoid concomitant use with ketoconazole.1 If concomitant use with other potent CYP3A inhibitors cannot be avoided, reduce initial abemaciclib dosage (200 or 150 mg twice daily depending on indication) to 100 mg twice daily or, in those already receiving a reduced dosage of abemaciclib (100 mg twice daily), reduce dosage of abemaciclib to 50 mg twice daily.1 If potent CYP3A inhibitor is discontinued, resume abemaciclib (after 3–5 terminal half-lives of the CYP3A inhibitor) at dosage used prior to initiation of potent CYP3A inhibitor.1 If used concomitantly with moderate CYP3A inhibitors, monitor for signs of abemaciclib toxicity and consider dosage modification for adverse reactions.1

Potent or moderate CYP3A inducers: Possible decreased systemic exposure to abemaciclib and its active metabolites and reduced efficacy of abemaciclib.1 Avoid concomitant use with potent or moderate CYP3A inducers; consider choosing alternative agent with no or minimal CYP3A induction potential.1

Specific Drugs and Foods

Drug

Interaction

Comments

Anastrozole

No effect on pharmacokinetics of anastrozole or abemaciclib1

Antifungals, azoles (e.g., itraconazole, ketoconazole)

Possible increased systemic exposure to abemaciclib, M-2, M-18, and M-20 and increased adverse effects1

Itraconazole: Simulations suggest 2.2-fold increase in potency-adjusted total AUC of unbound abemaciclib, M-2, M-18, and M-204

Ketoconazole: Simulations suggest increased AUC of abemaciclib by up to 16-fold1 4

Ketoconazole: Avoid concomitant use1

Other potent CYP3A inhibitors (e.g., itraconazole, posaconazole, voriconazole):4 Reduce initial abemaciclib dosage (200 or 150 mg twice daily depending on indication) to 100 mg twice daily; in those already receiving a reduced abemaciclib dosage (100 mg twice daily), reduce dosage to 50 mg twice daily1

If potent CYP3A inhibitor discontinued, resume abemaciclib (after 3–5 terminal half-lives of the CYP3A inhibitor) at dosage used prior to initiation of the CYP3A inhibitor1

Bosentan

Simulations suggest 41% decrease in potency-adjusted total AUC of unbound abemaciclib, M-2, M-18, and M-201

Avoid concomitant use1

Select alternative agent with less CYP3A induction potential1

Diltiazem

Simulations suggest approximate 2.4-fold increase in potency-adjusted total AUC of unbound abemaciclib, M-2, M-18, and M-201 4

Moderate CYP3A inhibitors (e.g., diltiazem): Monitor for abemaciclib toxicity and consider dosage modification1

Efavirenz

Simulations suggest 53% decrease in potency-adjusted total AUC of unbound abemaciclib, M-2, M-18, and M-201

Avoid concomitant use1

Select alternative agent with less CYP3A induction potential1

Exemestane

No effect on pharmacokinetics of exemestane or abemaciclib1

Fulvestrant

No effect on pharmacokinetics of fulvestrant or abemaciclib1

Grapefruit or grapefruit juice

Possible increased systemic exposure to abemaciclib1

Avoid concomitant use1

Letrozole

No effect on pharmacokinetics of letrozole or abemaciclib1

Loperamide

No effect on pharmacokinetics of loperamide or abemaciclib, M-2, or M-201

Macrolides (e.g., clarithromycin)

Possible increased systemic exposure to abemaciclib, M-2, M-18, and M-20 and increased adverse effects1

Clarithromycin: Increased potency-adjusted total AUC of unbound abemaciclib, M-2, and M-20 by 2.5-fold1

Reduce initial abemaciclib dosage (200 or 150 mg twice daily depending on indication) to 100 mg twice daily; in those already receiving reduced abemaciclib dosage (100 mg twice daily), reduce dosage to 50 mg twice daily1

If potent CYP3A inhibitor discontinued, resume abemaciclib (after 3–5 terminal half-lives of the CYP3A inhibitor) at dosage used prior to initiation of the CYP3A inhibitor1

Metformin

Increased peak plasma concentrations and AUC of metformin by 22 and 37%, respectively; reduced renal clearance and renal secretion of metformin by 45 and 62%, respectively1

Modafinil

Simulations suggest 29% decrease in potency-adjusted total AUC of unbound abemaciclib, M-2, M-18, and M-201

Avoid concomitant use1

Select alternative agent with less CYP3A induction potential1

Rifampin

Decreased potency-adjusted total AUC of unbound abemaciclib, M-2, M-18, and M-20 by approximately 70%1

Avoid concomitant use1

Select alternative agent with less CYP3A induction potential1

Tamoxifen

No effect on pharmacokinetics of tamoxifen or abemaciclib1

Verapamil

Simulations suggest approximate 1.6-fold increase in potency-adjusted total AUC of unbound abemaciclib, M-2, M-18, and M-201 4

Moderate CYP3A inhibitors (e.g., verapamil): Monitor for abemaciclib toxicity and consider dosage modification1

Abemaciclib Pharmacokinetics

Absorption

Bioavailability

Following oral administration, median time to peak plasma concentrations is 8 hours.1

AUC and peak plasma concentrations are dose proportional over dosage range of 50–200 mg; mean accumulation ratio is 3.2 or 2.3 based on AUC or peak plasma concentrations, respectively.1

Steady-state concentrations achieved in 5 days.1

Food

Administration with high-fat, high-calorie meal (approximately 800–1000 calories with over 50% of calories from fat) increases AUC and peak plasma concentrations of abemaciclib and its active metabolites by 9 and 26%, respectively.1

Special Populations

Mild, moderate, or severe (Child-Pugh class A, B, or C) hepatic impairment increases potency-adjusted total exposure to unbound abemaciclib and its active metabolites by 1.2-, 1.1-, or 2.4-fold, respectively; mean elimination half-life of abemaciclib prolonged by >twofold in patients with severe hepatic impairment.1

Mild or moderate renal impairment (Clcr 30–89 mL/minute) does not substantially affect systemic exposure.1 Data lacking for severe renal impairment (Clcr <30 mL/minute).1

Age (24–91 years), gender, and body weight (36–175 kg) do not substantially affect pharmacokinetics.1 15

Distribution

Extent

Not known whether distributed into human milk.1

CSF concentrations of abemaciclib and its active metabolites similar to unbound plasma concentrations in patients with advanced cancer.1

Plasma Protein Binding

>93% (mainly plasma proteins, albumin, α1-acid glycoprotein).1

Elimination

Metabolism

Principally metabolized by CYP3A4.1

Elimination Route

Eliminated in feces (81% of recovered dose [mainly as metabolites]) and urine (approximately 3%).1

Half-life

18.3 hours.1

Stability

Storage

Oral

Tablets

20–25°C (excursions permitted to 15–30°C).1

Actions

Advice to Patients

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Obtain abemaciclib through designated specialty pharmacies and authorized distributors.23

Abemaciclib

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

50 mg

Verzenio

Lilly

100 mg

Verzenio

Lilly

150 mg

Verzenio

Lilly

200 mg

Verzenio

Lilly

AHFS DI Essentials™. © Copyright 2024, Selected Revisions August 24, 2023. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Eli Lilly and Company. Verzenio (abemaciclib) tablets prescribing information. Indianapolis, IN; 2023 Mar. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=be4bc0de-0fdc-4d46-8d25-be43c79e6a06

2. Sledge GW, Toi M, Neven P et al. MONARCH 2: Abemaciclib in Combination With Fulvestrant in Women With HR+/HER2- Advanced Breast Cancer Who Had Progressed While Receiving Endocrine Therapy. J Clin Oncol. 2017; 35:2875-2884. http://www.ncbi.nlm.nih.gov/pubmed/28580882?dopt=AbstractPlus

3. Dickler MN, Tolaney SM, Rugo HS et al. MONARCH 1, A Phase II Study of Abemaciclib, a CDK4 and CDK6 Inhibitor, as a Single Agent, in Patients with Refractory HR/HER2Metastatic Breast Cancer. Clin Cancer Res. 2017; 23:5218-5224. http://www.ncbi.nlm.nih.gov/pubmed/28533223?dopt=AbstractPlus

4. Food and Drug Administration. Center for Drug Evaluation and Research. Application number 208716Orig1s000: Multi-discipline review. From FDA website. Accessed 2018 Mar 8. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208716Orig1s000MultidisciplineR.pdf

5. Morikawa A, Henry NL. Palbociclib for the Treatment of Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer. Clin Cancer Res. 2015; 21:3591-6. http://www.ncbi.nlm.nih.gov/pubmed/26100274?dopt=AbstractPlus

6. Rocca A, Farolfi A, Bravaccini S et al. Palbociclib (PD 0332991) : targeting the cell cycle machinery in breast cancer. Expert Opin Pharmacother. 2014; 15:407-20. http://www.ncbi.nlm.nih.gov/pubmed/24369047?dopt=AbstractPlus

7. Murphy CG, Dickler MN. The Role of CDK4/6 Inhibition in Breast Cancer. Oncologist. 2015; 20:483-90. http://www.ncbi.nlm.nih.gov/pubmed/25876993?dopt=AbstractPlus

8. Mangini NS, Wesolowski R, Ramaswamy B et al. Palbociclib: A Novel Cyclin-Dependent Kinase Inhibitor for Hormone Receptor-Positive Advanced Breast Cancer. Ann Pharmacother. 2015; 49:1252-60. http://www.ncbi.nlm.nih.gov/pubmed/26324355?dopt=AbstractPlus

9. Vidula N, Rugo HS. Cyclin-Dependent Kinase 4/6 Inhibitors for the Treatment of Breast Cancer: A Review of Preclinical and Clinical Data. Clin Breast Cancer. 2016; 16:8-17. http://www.ncbi.nlm.nih.gov/pubmed/26303211?dopt=AbstractPlus

10. Hosford SR, Miller TW. Clinical potential of novel therapeutic targets in breast cancer: CDK4/6, Src, JAK/STAT, PARP, HDAC, and PI3K/AKT/mTOR pathways. Pharmgenomics Pers Med. 2014; 7:203-15. http://www.ncbi.nlm.nih.gov/pubmed/25206307?dopt=AbstractPlus

11. Finn RS, Dering J, Conklin D et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009; 11:R77. http://www.ncbi.nlm.nih.gov/pubmed/19874578?dopt=AbstractPlus

12. Sutherland RL, Musgrove EA. CDK inhibitors as potential breast cancer therapeutics: new evidence for enhanced efficacy in ER+ disease. Breast Cancer Res. 2009; 11:112. http://www.ncbi.nlm.nih.gov/pubmed/20067604?dopt=AbstractPlus

13. DeMichele A, Clark AS, Tan KS et al. CDK 4/6 inhibitor palbociclib (PD0332991) in Rb+ advanced breast cancer: phase II activity, safety, and predictive biomarker assessment. Clin Cancer Res. 2015; 21:995-1001. http://www.ncbi.nlm.nih.gov/pubmed/25501126?dopt=AbstractPlus

14. Goetz MP, Toi M, Campone M et al. MONARCH 3: Abemaciclib As Initial Therapy for Advanced Breast Cancer. J Clin Oncol. 2017; 35:3638-3646. http://www.ncbi.nlm.nih.gov/pubmed/28968163?dopt=AbstractPlus

15. Tate SC, Sykes AK, Kulanthaivel P et al. A Population Pharmacokinetic and Pharmacodynamic Analysis of Abemaciclib in a Phase I Clinical Trial in Cancer Patients. Clin Pharmacokinet. 2018; 57:335-344. http://www.ncbi.nlm.nih.gov/pubmed/28540640?dopt=AbstractPlus

16. Torres-Guzmán R, Calsina B, Hermoso A et al. Preclinical characterization of abemaciclib in hormone receptor positive breast cancer. Oncotarget. 2017; 8:69493-69507. http://www.ncbi.nlm.nih.gov/pubmed/29050219?dopt=AbstractPlus

17. Food and Drug Administration. Drug safety communication: FDA warns about rare but severe lung inflammation with Ibrance, Kisqali, and Verzenio for breast cancer. Silver Spring, MD; 2019 Sept 13. From FDA website. https://www.fda.gov/drugs/drug-safety-and-availability/fda-warns-about-rare-severe-lung-inflammation-ibrance-kisqali-and-verzenio-breast-cancer

18. Johnston S, Martin M, Di Leo A et al. MONARCH 3 final PFS: a randomized study of abemaciclib as initial therapy for advanced breast cancer. NPJ Breast Cancer. 2019; 5:5. http://www.ncbi.nlm.nih.gov/pubmed/30675515?dopt=AbstractPlus

19. Sledge GW, Toi M, Neven P et al. The Effect of Abemaciclib Plus Fulvestrant on Overall Survival in Hormone Receptor-Positive, ERBB2-Negative Breast Cancer That Progressed on Endocrine Therapy-MONARCH 2: A Randomized Clinical Trial. JAMA Oncol. 2019; http://www.ncbi.nlm.nih.gov/pubmed/31563959?dopt=AbstractPlus

20. Johnston SRD, Harbeck N, Hegg R et al. Abemaciclib Combined With Endocrine Therapy for the Adjuvant Treatment of HR+, HER2-, Node-Positive, High-Risk, Early Breast Cancer (monarchE). J Clin Oncol. 2020; 38:3987-3998. http://www.ncbi.nlm.nih.gov/pubmed/32954927?dopt=AbstractPlus

21. Harbeck N, Rastogi P, Martin M et al. Adjuvant abemaciclib combined with endocrine therapy for high-risk early breast cancer: updated efficacy and Ki-67 analysis from the monarchE study. Ann Oncol. 2021; 32:1571-1581. http://www.ncbi.nlm.nih.gov/pubmed/34656740?dopt=AbstractPlus

22. Neven P, Rugo HS, Tolaney SM et al. Abemaciclib plus fulvestrant in hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer in premenopausal women: subgroup analysis from the MONARCH 2 trial. Breast Cancer Res. 2021; 23:87. http://www.ncbi.nlm.nih.gov/pubmed/34425869?dopt=AbstractPlus

23. Eli Lilly and Company. Verzenio: access and support. From Eli Lilly and Company for US Healthcare Professionals website. Accessed 2022 Apr 18. https://www.verzenio.com/hcp/access-support

24. Institute for Safe Medication Practices. ISMP list of high-alert medications in acute care settings. https://www.ismp.org/sites/default/files/attachments/2018-08/highAlert2018-Acute-Final.pdf. Accessed 2023 Aug 23.

70. Burstein HJ, Somerfield MR, Barton DL et al. Endocrine Treatment and Targeted Therapy for Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Metastatic Breast Cancer: ASCO Guideline Update. J Clin Oncol. 2021; 39:3959-3977. http://www.ncbi.nlm.nih.gov/pubmed/34324367?dopt=AbstractPlus

71. Giordano SH, Freedman RA, Somerfield MR et al. Abemaciclib With Endocrine Therapy in the Treatment of High-Risk Early Breast Cancer: ASCO Optimal Adjuvant Chemotherapy and Targeted Therapy Guideline Rapid Recommendation Update. J Clin Oncol. 2022; 40:307-309. http://www.ncbi.nlm.nih.gov/pubmed/34878801?dopt=AbstractPlus

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