Abemaciclib (abemaciclib)
Abemaciclib is a cdk4/6 inhibitor (cyclin-dependent kinase 4/6 inhibitor); kinase inhibitor from Eli Lilly and Company (Lilly USA, LLC), marketed originally as Verzenio. This monograph covers approved indications, mechanism, dosing, side effects and the manufacturer landscape.
Overview
Abemaciclib (Verzenio) is an oral, continuously dosed CDK4/6 inhibitor used across the whole spectrum of hormone receptor (HR)-positive, HER2-negative breast cancer, from high-risk early disease after surgery to advanced and metastatic disease. Like palbociclib it blocks cyclin-dependent kinases 4 and 6, the enzymes that partner with cyclin D1 to phosphorylate the retinoblastoma protein and push a cell through the G1 checkpoint into DNA synthesis. In ER-positive breast cancer cell lines continuous exposure to abemaciclib inhibits Rb phosphorylation, arrests cells in G1 and triggers senescence and apoptosis. What distinguishes abemaciclib from its class-mates is its dosing and toxicity profile. It is given without a treatment break, at 150 mg twice daily in combination with fulvestrant, tamoxifen or an aromatase inhibitor, or 200 mg twice daily as monotherapy for patients who have progressed after endocrine therapy and prior chemotherapy in the metastatic setting. In early breast cancer it is combined with endocrine therapy for a total of two years. Its signature adverse effect is diarrhoea, which affects 81-90% of patients and is grade 3 in 8-20% - far more common than with palbociclib - and requires early loperamide and fluid management. Neutropenia is less frequent and less deep than with palbociclib (37-46%, grade 3 or worse 19-32%), but hepatotoxicity, interstitial lung disease/pneumonitis and venous thromboembolic events are additional risks. Blood counts and liver enzymes are checked every two weeks for the first two months, then monthly for two months. Abemaciclib remains patent-protected in the US and EU, so no FDA- or EMA-approved generic exists. These are nationally registered products, not FDA/EMA generics, and no bioequivalence study against Verzenio has been published.
How it works
Abemaciclib blocks CDK4 and CDK6, two proteins that drive cancer cells through the cell cycle. This stops hormone-receptor-positive breast cancer cells from dividing. It is used in early breast cancer after surgery (adjuvant setting) and in advanced or metastatic disease, either with hormone therapy or on its own.
Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins. In estrogen receptor-positive (ER+) breast cancer cell lines, cyclin D1 and CDK4/6 promote phosphorylation of the retinoblastoma protein (Rb), cell cycle progression, and cell proliferation. In vitro, continuous exposure to abemaciclib inhibited Rb phosphorylation and blocked progression from G1 into S phase of the cell cycle, resulting in senescence and apoptosis. (FDA label, section 12. 1)
Approved indications
- In combination with endocrine therapy (tamoxifen or an aromatase inhibitor) for the adjuvant treatment of adults with HR-positive, HER2-negative, node-positive, early breast cancer at high risk of recurrence
- In combination with an aromatase inhibitor as initial endocrine-based therapy for adults with HR-positive, HER2-negative advanced or metastatic breast cancer
- In combination with fulvestrant for adults with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy
- As monotherapy for adults with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting
Dosage & administration
150 mg orally twice daily in combination with fulvestrant, tamoxifen or an aromatase inhibitor; 200 mg orally twice daily as monotherapy. Tablets taken with or without food. For early breast cancer, continue until completion of 2 years of treatment, disease recurrence, or unacceptable toxicity; for advanced/metastatic disease, until disease progression or unacceptable toxicity.
Dose adjustment
Combination dose level: starting 150 mg twice daily, first reduction 100 mg twice daily, second reduction 50 mg twice daily. Monotherapy dose level: starting 200 mg twice daily, first reduction 150 mg, second 100 mg, third 50 mg twice daily; discontinue if 50 mg twice daily is not tolerated. With strong CYP3A inhibitors (other than ketoconazole, which should be avoided), reduce to 100 mg twice daily. Severe hepatic impairment (Child-Pugh C): reduce dosing frequency to once daily.
Side effects
Diarrhea (81%-90%; Grade 3 in 8%-20%) · Neutropenia (37%-46%; Grade >=3 in 19%-32%) · Nausea · Abdominal pain · Infections · Fatigue (41%) · Anemia · Leukopenia · Decreased appetite (12%) · Vomiting · Headache (20%) · Alopecia (11%)
- Thrombocytopenia
- Hepatotoxicity (Grade >=3 ALT 2%-6%, AST 2%-3%)
- Interstitial lung disease / pneumonitis (3%-3. 3% any grade)
- Venous thromboembolic events (2%-5%)
Monitoring
- Complete blood counts prior to start, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated
- Liver function tests (ALT, AST, serum bilirubin) prior to start, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated
- Monitoring for diarrhea at the first sign of loose stools; start antidiarrheal therapy (e. g. loperamide) and increase oral fluids
- Monitoring for pulmonary symptoms of ILD/pneumonitis (hypoxia, cough, dyspnea, interstitial infiltrates)
- Monitoring for signs and symptoms of venous thrombosis and pulmonary embolism
Generic and biosimilar landscape
Bangladeshi products (Everest Abemaxen, Beacon Abeza, Eskayef Abeclib) are national DGDA-registered products made under the TRIPS least-developed-country patent exemption, not FDA/EMA-approved generics. No published bioequivalence study against Verzenio was found for these brands. Note: the task brief referred to an Everest abemaciclib brand named 'Abexinib'; no source confirming that name was found - Everest's own product list shows 'Abemaxen 150' and 'Abemaxen 200'.
Who makes it
| Manufacturer | Country | Brand | Strength | Notes |
|---|---|---|---|---|
| Everest Pharmaceuticals Ltd. | Bangladesh | Abemaxen | 150 mg and 200 mg tablets | Listed on Everest's own product pages (Abemaxen 150, Abemaxen 200). Name 'Abexinib' from the brief could not be verified |
| Beacon Pharmaceuticals PLC | Bangladesh | Abeza | 150 mg and 200 mg tablets | Unit the data (150 mg) and (200 mg) on MedEx |
| Eskayef Pharmaceuticals Ltd. | Bangladesh | Abeclib | 150 mg and 200 mg tablets | Unit the data (150 mg) and (200 mg) on MedEx |
| Healthcare Pharmaceuticals Ltd. | Bangladesh | Abezino | 150 mg and 200 mg tablets | Listed on MedEx |
Availability in Southeast Asia
| Country | Status | Notes |
|---|---|---|
| Singapore | approved | HSA new drug indication approval dated 28/05/2024 for VERZENIO FILM-COATED TABLET 50MG/100MG/150MG and YULAREB film-coated tablets (registrant DKSH Singapore Pte Ltd) |
| Malaysia | marketed | Abemaciclib is named by NPRA among the CDK4/6 inhibitors in use in Malaysia (NPRA safety alert on severe lung inflammation) |
| Thailand | No public source confirming abemaciclib registration found in this research | |
| Philippines | No public source confirming abemaciclib registration found in this research | |
| Indonesia | No public source confirming abemaciclib registration (BPOM) found in this research | |
| Vietnam | No public source confirming abemaciclib registration found in this research |
Frequently asked questions
Is Abemaxen the same as Verzenio?
Bangladeshi products (Everest Abemaxen, Beacon Abeza, Eskayef Abeclib) are national DGDA-registered products made under the TRIPS least-developed-country patent exemption, not FDA/EMA-approved generics. No published bioequivalence study against Verzenio was found for these brands. Note: the task brief referred to an Everest abemaciclib brand named 'Abexinib'; no source confirming that name was found - Everest's own product list shows 'Abemaxen 150' and 'Abemaxen 200'. Manufacturers supplying abemaciclib generic versions include Beacon Pharmaceuticals PLC, Eskayef Pharmaceuticals Ltd. , Everest Pharmaceuticals Ltd. , Healthcare Pharmaceuticals Ltd. . Brands registered in Bangladesh include Abeclib, Abeza, Abezino.
What is the difference between abemaciclib and palbociclib?
Abemaciclib (CDK4/6 inhibitor (cyclin-dependent kinase 4/6 inhibitor); kinase inhibitor, originally Verzenio by Eli Lilly and Company (Lilly USA, LLC)) Abemaciclib blocks CDK4 and CDK6, two proteins that drive cancer cells through the cell cycle. This stops hormone-receptor-positive breast cancer cells from dividing. It is used in early breast cancer after surgery (adjuvant setting) and in advanced or metastatic disease, either with hormone therapy or on its own. 150 mg orally twice daily in combination with fulvestrant, tamoxifen or an aromatase inhibitor; 200 mg orally twice daily as monotherapy. Tablets taken with or without food. For early breast cancer, continue until completion of 2 years of treatment, disease recurrence, or unacceptable toxicity; for advanced/metastatic disease, until disease progression or unacceptable toxicity.
How long do you take abemaciclib for early breast cancer?
Abemaciclib (CDK4/6 inhibitor (cyclin-dependent kinase 4/6 inhibitor); kinase inhibitor, originally Verzenio by Eli Lilly and Company (Lilly USA, LLC)) Abemaciclib blocks CDK4 and CDK6, two proteins that drive cancer cells through the cell cycle. This stops hormone-receptor-positive breast cancer cells from dividing. It is used in early breast cancer after surgery (adjuvant setting) and in advanced or metastatic disease, either with hormone therapy or on its own. 150 mg orally twice daily in combination with fulvestrant, tamoxifen or an aromatase inhibitor; 200 mg orally twice daily as monotherapy. Tablets taken with or without food. For early breast cancer, continue until completion of 2 years of treatment, disease recurrence, or unacceptable toxicity; for advanced/metastatic disease, until disease progression or unacceptable toxicity.
How do you manage diarrhea from abemaciclib?
Abemaciclib (CDK4/6 inhibitor (cyclin-dependent kinase 4/6 inhibitor); kinase inhibitor, originally Verzenio by Eli Lilly and Company (Lilly USA, LLC)) Abemaciclib blocks CDK4 and CDK6, two proteins that drive cancer cells through the cell cycle. This stops hormone-receptor-positive breast cancer cells from dividing. It is used in early breast cancer after surgery (adjuvant setting) and in advanced or metastatic disease, either with hormone therapy or on its own. 150 mg orally twice daily in combination with fulvestrant, tamoxifen or an aromatase inhibitor; 200 mg orally twice daily as monotherapy. Tablets taken with or without food. For early breast cancer, continue until completion of 2 years of treatment, disease recurrence, or unacceptable toxicity; for advanced/metastatic disease, until disease progression or unacceptable toxicity.
Does abemaciclib cause low white blood cell counts?
Recommended monitoring for abemaciclib: Complete blood counts prior to start, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated; Liver function tests (ALT, AST, serum bilirubin) prior to start, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated; Monitoring for diarrhea at the first sign of loose stools; start antidiarrheal therapy (e. g. loperamide) and increase oral fluids; Monitoring for pulmonary symptoms of ILD/pneumonitis (hypoxia, cough, dyspnea, interstitial infiltrates); Monitoring for signs and symptoms of venous thrombosis and pulmonary embolism
Is abemaciclib approved in Singapore?
Abemaciclib (CDK4/6 inhibitor (cyclin-dependent kinase 4/6 inhibitor); kinase inhibitor, originally Verzenio by Eli Lilly and Company (Lilly USA, LLC)) Abemaciclib blocks CDK4 and CDK6, two proteins that drive cancer cells through the cell cycle. This stops hormone-receptor-positive breast cancer cells from dividing. It is used in early breast cancer after surgery (adjuvant setting) and in advanced or metastatic disease, either with hormone therapy or on its own. 150 mg orally twice daily in combination with fulvestrant, tamoxifen or an aromatase inhibitor; 200 mg orally twice daily as monotherapy. Tablets taken with or without food. For early breast cancer, continue until completion of 2 years of treatment, disease recurrence, or unacceptable toxicity; for advanced/metastatic disease, until disease progression or unacceptable toxicity.
Can abemaciclib be taken as a single agent without hormone therapy?
Abemaciclib (CDK4/6 inhibitor (cyclin-dependent kinase 4/6 inhibitor); kinase inhibitor, originally Verzenio by Eli Lilly and Company (Lilly USA, LLC)) Abemaciclib blocks CDK4 and CDK6, two proteins that drive cancer cells through the cell cycle. This stops hormone-receptor-positive breast cancer cells from dividing. It is used in early breast cancer after surgery (adjuvant setting) and in advanced or metastatic disease, either with hormone therapy or on its own. 150 mg orally twice daily in combination with fulvestrant, tamoxifen or an aromatase inhibitor; 200 mg orally twice daily as monotherapy. Tablets taken with or without food. For early breast cancer, continue until completion of 2 years of treatment, disease recurrence, or unacceptable toxicity; for advanced/metastatic disease, until disease progression or unacceptable toxicity.
What is the starting dose of abemaciclib and can it be reduced?
Standard dosing for abemaciclib: 150 mg orally twice daily in combination with fulvestrant, tamoxifen or an aromatase inhibitor; 200 mg orally twice daily as monotherapy. Tablets taken with or without food. For early breast cancer, continue until completion of 2 years of treatment, disease recurrence, or unacceptable toxicity; for advanced/metastatic disease, until disease progression or unacceptable toxicity. Dose adjustments: Combination dose level: starting 150 mg twice daily, first reduction 100 mg twice daily, second reduction 50 mg twice daily. Monotherapy dose level: starting 200 mg twice daily, first reduction 150 mg, second 100 mg, third 50 mg twice daily; discontinue if 50 mg twice daily is not tolerated. With strong CYP3A inhibitors (other than ketoconazole, which should be avoided), reduce to 100 mg twice daily. Severe hepatic impairment (Child-Pugh C): reduce dosing frequency to once daily.
Does abemaciclib increase the risk of blood clots?
Recommended monitoring for abemaciclib: Complete blood counts prior to start, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated; Liver function tests (ALT, AST, serum bilirubin) prior to start, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated; Monitoring for diarrhea at the first sign of loose stools; start antidiarrheal therapy (e. g. loperamide) and increase oral fluids; Monitoring for pulmonary symptoms of ILD/pneumonitis (hypoxia, cough, dyspnea, interstitial infiltrates); Monitoring for signs and symptoms of venous thrombosis and pulmonary embolism
Sources
- https://www.accessdata.fda.gov/drugsatfda_docs/label/2026/208716s021lbl.pdf
- https://www.fda.gov/drugs/resources-information-approved-drugs/fda-expands-early-breast-cancer-indication-abemaciclib-endocrine-therapy
- https://medex.com.bd/generics/2043/abemaciclib
- https://medex.com.bd/generics/2043/abemaciclib/brand-names
- https://www.everestpharmabd.com/products/Oncology
- https://www.everestpharmabd.com/product_details/1860
- https://www.hsa.gov.sg/announcements/new-drug-indication-approval---may-2024
- https://www.drugs.com/history/verzenio.html
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