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Abemaciclib

Alias: Abemaciclib; LY2835219; LY-2835219; LY 2835219; Abemaciclib methanesulfonate; Verzenio; LY2835219 free base; LY-2835219; UNII-60UAB198HK; Verzenios; LY2835219 methanesulfonate
Cat No.:V3692 Purity: ≥98%
Abemaciclib (formerly known as LY2835219; trade name:Verzenio) is a potent and selective, and orally bioavailable dual inhibitor of CDK4 (cyclin-dependent kinase) and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
Abemaciclib
Abemaciclib Chemical Structure CAS No.: 1231929-97-7
Product category: CDK
This product is for research use only, not for human use. We do not sell to patients.
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100mg
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1g
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Other Forms of Abemaciclib:

  • Abemaciclib (LY2835219) mesylate
  • Abemaciclib-d8 (LY2835219-d8)
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's Abemaciclib has been cited by 1 publication
Purity & Quality Control Documentation

Purity: =99.4%

Purity: =99.6%

Product Description

Abemaciclib (formerly known as LY2835219; trade name: Verzenio) is a potent and selective, and orally bioavailable dual inhibitor of CDK4 (cyclin-dependent kinase) and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Abemaciclib received FDA approval in September 2017 to treat specific advanced or metastatic breast cancers. Early G1 retinoblastoma (Rb) protein phosphorylation is inhibited by LY2835219, which specifically inhibits CDK4 and 6. By stopping CDK-mediated G1-S phase transition, inhibition of Rb phosphorylation stops the cell cycle in the G1 phase, inhibiting DNA synthesis and slowing the growth of cancer cells. As observed in some cancer forms, overexpression of the serine/threonine kinases CDK4/6 can result in cell cycle dysregulation.

Biological Activity I Assay Protocols (From Reference)
Targets
Cdk4/cyclin D1 (IC50 = 2 nM); CDK6/cyclinD1 (IC50 = 10 nM); CDK9/cyclinT1 (IC50 = 57 nM); CDK5/p35 (IC50 = 287 nM); Cdk5/p25 (IC50 = 355 nM); CDK2/cyclinE (IC50 = 504 nM); CDK7/Mat1/cyclinH1 (IC50 = 3910 nM); CDK1/cyclinB1 (IC50 = 1627 nM); PIM1 (IC50 = 39 nM); PIM2 (IC50 = 3400 nM); HIPK2 (IC50 = 31 nM); DYRK2 (IC50 = 61 nM); CK2 (IC50 = 117 nM); GSK3b (IC50 = 192 nM); JNK3 (IC50 = 389 nM); FLT3 (D835Y) (IC50 = 403 nM); FLT3 (IC50 = 3960 nM); DRAK1 (IC50 = 659 nM)
ln Vitro

In vitro activity: Abemaciclib (formerly known as LY2835219) is a potent and selective, orally available dual inhibitor of CDK4 (cyclin-dependent kinase) and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6 can cause cell cycle deregulation as seen in certain types of cancer.


Kinase Assay: Cells (5 × 103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturers instructions and a luminescence plate reader.


Cell Assay: Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturers instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of < 1 is synergistic and a CI of > 1 is antagonistic.

ln Vivo
Abemaciclib exhibits both single-agent antitumor activity and durable cell-cycle inhibition in a colorectal cancer xenograft model that was used to create an integrated pharmacokinetic/pharmacodynamic model. Abemaciclib can be dosed orally on a continuous schedule to achieve sustained target inhibition. Numerous other human cancer xenograft models, such as those derived from melanoma, glioblastoma, mantle cell lymphoma, and non-small cell lung cancer (NSCLC), show tumor growth inhibition. In an intracranial glioblastoma xenograft model, bemaciclib diffuses across the blood–brain barrier and increases survival time. Abemaciclib's pharmacokinetics in humans indicate a slow absorption phase, with a median of 4 to 6 hours between the oral dose and the maximum plasma concentration (tmax). It is distributed and cleared thoroughly. The average terminal elimination half-life (t1/2) varied between 17.4 and 38.1 hours, and there was no discernible shift in clearance that was dose-dependent[2].
Abemaciclib monotherapy resulted in tumor growth delay that was associated with an increased T cell inflammatory signature in tumors. Combination with anti-PD-L1 therapy led to complete tumor regressions and immunological memory, accompanied by enhanced antigen presentation, a T cell inflamed phenotype, and enhanced cell cycle control. [3]
Researchers evaluated the safety, pharmacokinetic profile, pharmacodynamic effects, and antitumor activity of abemaciclib, an orally bioavailable inhibitor of cyclin-dependent kinases (CDK) 4 and 6, in a multicenter study including phase I dose escalation followed by tumor-specific cohorts for breast cancer, non-small cell lung cancer (NSCLC), glioblastoma, melanoma, and colorectal cancer. A total of 225 patients were enrolled: 33 in dose escalation and 192 in tumor-specific cohorts. Dose-limiting toxicity was grade 3 fatigue. The maximum tolerated dose was 200 mg every 12 hours. The most common possibly related treatment-emergent adverse events involved fatigue and the gastrointestinal, renal, or hematopoietic systems. Plasma concentrations increased with dose, and pharmacodynamic effects were observed in proliferating keratinocytes and tumors. Radiographic responses were achieved in previously treated patients with breast cancer, NSCLC, and melanoma. For hormone receptor-positive breast cancer, the overall response rate was 31%; moreover, 61% of patients achieved either response or stable disease lasting ≥6 months. [2]
Enzyme Assay
LY2835219 (abemaciclib) was identified via compound and biochemical screening by scientists at Eli Lilly and Company Research Laboratories and selected for its biological activity and highly selective inhibition of the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK/cyclin complexes or cell-cycle-related kinases within the nanomolar ranges, except for inhibition of CDK9 at IC50 at least five times higher (Figure 2).23 The compound was shown to act as a competitive inhibitor of the ATP-binding domain of the CDK4 and CDK6 and to be 14 times more potent against CDK4 than against CDK6.24 In comparison to palbociclib and ribociclib, abemaciclib shows higher selectivity for the complex CDK4/cyclin D1, with IC50 values five times lower than those of the two other compounds [1].
Cell Assay
The 96-well plate is seeded with cells, which are then left to adhere for an entire night before being treated for 72 hours with either the indicated compounds or DMSO control (0.1% v/v). A Cell Counting Kit is used, as directed by the manufacturer, to assess the viability and proliferation of cells. CompuSyn is used to analyze the relationship between mTOR inhibitor and abemaciclib. An additive drug interaction is indicated by a combination index (CI) value of 1, while a synergistic or antagonistic drug interaction is indicated by a CI value of <1 or >1.
In Vitro Treatment of Human Breast Carcinoma and T Cells [3]
Breast cancer cell lines MCF-7 and MDA-MB-46 were treated with DMSO and abemaciclib (500 nM) for 8 days. RNA was isolated as described above. Jurkat T cells or primary human T cells were stimulated with anti-CD3/CD28/CD2 or thapsigargin and incubated with abemaciclib as indicated. Primary human T cells were isolated from whole blood by negative selection using RosetteSep kits. T cells were cultured in RPMI1640 supplemented with 10% fetal calf serum (FCS), 100 U/mL penicillin, 100 μg/mL streptomycin, 10 mM HEPES, and 2 mM L-glutamine and stimulated with CD3/CD28 DynaBeads at a 1:3 T cell/bead ratio. Abemaciclib was added at 0.3 μM final concentration. Cells were counted and fed fresh media every 2–3 days.
In Vitro Tumor Cell Viability Assay [3]
Tumor cells were cultured for 4 hr alone at 37°C, and then abemaciclib, palbociclib, or DMSO control was added at indicated concentrations for 96 hr at 37°C. Cell viability was then assessed using CellTiter-Glo. Cell viability inhibition (%) was calculated according to the formula [1 − (mean luminosity of treated sample/mean luminosity of untreated control)] × 100. Fifty-percent inhibitory concentration (IC50) for growth or viability inhibition was calculated using a four-parameter logistic curve fit formula.
NFAT Reporter Assay [3]
Jurkat T cells containing an NFAT-luc reporter gene were incubated with abemaciclib at the indicated concentrations for 30 min and then stimulated with 250 ng/mL of anti-CD3/CD28/CD2 for 6 hr. NFAT-luc activity was monitored using Luciferase Assay Reagent in a Wallac 1420 Victor2 Multilabel Counter. NFAT stimulation (%) was calculated using untreated control samples.
Animal Protocol
Subcutaneous injections of OSC-19 (1×106) cells are given to six-week-old BALB/c female nude mice. Mice are randomized by tumor size and given each treatment when tumor sizes approach 100 mm3. Each treatment group comprises a minimum of 5 mice. Every group of mice receives a daily oral gavage dose of either RAD001 (5 mg/kg/d), Abemaciclib (45 mg/kg/d or 90 mg/kg/d), or a combination of both. In 20 mM phosphate buffer (pH 2.0), 1% HEC is used to dissolve the Abemaciclib. Weight and tumor size are measured twice a week. V=(L×W2)/2 is the formula used to compute tumor volumes. On day 14, mice undergo one last gavage before being sacrificed the next day. In order to perform immunohistochemistry and Western blot, the tumors are removed.
In Vivo Tumor Studies [2]
BALB/c or C57BL/6 mice were implanted into the flank subcutaneously with 1 × 106 CT26, 5 × 105 MC38, or 5 × 105 EMT6 tumor cells per mouse on day 0. Mice were randomized into individual treatment groups (n = 5–15 mice per group) as indicated. A separate cohort of animals (n = 5 animals per time point) was allocated for mechanistic analyses in some cases. Abemaciclib was used. Rat anti-mouse anti-PD-L1 was generated from a rat of Lou/WS1 strain immunized with recombinant mouse PD-L1-Fc protein. 178G7 was identified on the basis of its binding to PD-L1 (half maximal effective concentration [EC50] = 0.1 nM) and blocking activities against PD-L1 interactions with PD-1 and CD80 (IC50 = 1.5 nM and 2.5 nM, respectively). Tumor volume (TV) was calculated as TV (mm3) = π/6 × length × width2. Animals were sacrificed because of progressive disease if tumor burden was greater than 2,500 mm3 or growth would surpass 2,500 mm3 before the next measurement. For experiments with secondary tumor re-challenge, mice were re-challenged with 1 × 106 CT26 tumors on the opposite flank of the original tumor injection site. Secondary challenge tumor growth was followed for up to 22 days.
ADME/Pharmacokinetics
Absorption, Distribution and Excretion
The plasma concentration of the drug increases in a dose-proportional manner. Following a single oral dose administration of 200 mg abemaciclib, the mean peak plasma concentration (Cmax) of 158 ng/mL is reached after 6 hours. The median time to reach maximum plasma concentration (Tmax) ranges from 4-6 hours following an oral administration of abemaciclib over a range of 50–275 mg, but may range up to 24 hours. The absolute bioavailability of the drug is reported to be 45%.
Following a single oral dose of 150mg radiolabeled abemaciclib, approximately 81% of the total dose was recovered in feces while 3% of the dose was detected in urine. The majority of the drug is exceted as metabolites.
The geometric mean systemic volume of distribution is approximately 690.3 L (49% CV).
The geometric mean hepatic clearance (CL) of abemaciclib in patients was 26.0 L/h (51% CV).
Metabolism / Metabolites
Abemaciclib mainly undergoes hepatic metabolism mediated by CYP3A4. The major metabolite formed is N-desethylabemaciclib (M2), while other metabolites hydroxyabemaciclib (M20), hydroxy-N-desethylabemaciclib (M18), and an oxidative metabolite (M1) are also formed. M2, M18, and M20 are equipotent to abemaciclib and their AUCs accounted for 25%, 13%, and 26% of the total circulating analytes in plasma, respectively.
Biological Half-Life
The mean plasma elimination half-life for abemaciclib in patients was 18.3 hours (72% CV).
Toxicity/Toxicokinetics
Hepatotoxicity
In the large clinical trials, adverse events were common and led to dose reductions in up to one-half of patients and discontinuation in 9%. In preregistration clinical trials, ALT elevations occurred in 31% to 41% of abemaciclib treated subjects which were above 5 times the ULN in 3% to 5%. In one study, several recipients developed clinically apparent liver injury with jaundice and one recipient died of hepatic failure, but these outcomes were considered to be unrelated to abemaciclib therapy. Thus, there were no cases of clinically apparent liver injury that could be attributed to abemaciclib therapy during prelicensure studies. Since the approval and more widescale use of abemaciclib, there have been no published reports of its hepatotoxicity. Nevertheless, the high rate of serum enzyme elevations during therapy and the similarity of abemaciclib to ribociclib and palbociclib makes it an agent that should be suspected of causing rare instances of clinically significant liver injury.
Likelihood score: E* (unproved but suspected, rare cause of clinically apparent liver injury).
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the clinical use of abemaciclib during breastfeeding. Because abemaciclib and its metabolites are over 90% bound to plasma proteins, the amount in milk is likely to be low. However, the manufacturer recommends that breastfeeding be discontinued during abemaciclib therapy and for 3 weeks after the final dose.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
Protein Binding
According to in vitro models using animal brain tissues, the protein binding of abemaciclib is approximately 95-98%. While abemaciclib demonstrated *in vitro* binding to serum albumin, alpha-1-acid glycoprotein and other human plasma proteins in a concentration-depedent manner, its major metabolites are also shown to bind to plasms proteins as well. The approximate bound fractions of M2, M18 and M20 are 93.4%, 96.8% and 97.8%, respectively.
References

[1]. Drug Des Devel Ther . 2018 Feb 16:12:321-330.

[2]. Cancer Discov . 2016 Jul;6(7):740-53.

[3]. Cell Rep . 2018 Mar 13;22(11):2978-2994.

Additional Infomation
Pharmacodynamics
In combination with fulvestrant, the progression-free survival for patients with HR-positive, HER2-negative breast cancer was 16.4 months compared to 9.3 months for patients taking a placebo with fulvestrant. As a monotherapy, 19.7% of patients taking abemaciclib achieved complete or partial shrinkage of their tumors for a median 8.6 months after treatment. Abemaciclib induces cell cycle arrest and exerts an antitumor activity in human tumor xenograft models. In patient investigations and a healthy volunteer study, abemaciclib is not shown to induce any clinically significant changes in the QTc interval.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H32F2N8
Molecular Weight
506.59
Exact Mass
506.271
Elemental Analysis
C, 64.01; H, 6.37; F, 7.50; N, 22.12
CAS #
1231929-97-7
Related CAS #
Abemaciclib methanesulfonate;1231930-82-7;Abemaciclib-d8;2088650-53-5
PubChem CID
46220502
Appearance
White to off-white solid powder
Density
1.3±0.1 g/cm3
Boiling Point
689.3±65.0 °C at 760 mmHg
Flash Point
370.7±34.3 °C
Vapour Pressure
0.0±2.2 mmHg at 25°C
Index of Refraction
1.656
LogP
2.74
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
9
Rotatable Bond Count
7
Heavy Atom Count
37
Complexity
723
Defined Atom Stereocenter Count
0
SMILES
CC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C
InChi Key
UZWDCWONPYILKI-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H32F2N8/c1-5-35-8-10-36(11-9-35)16-19-6-7-24(30-14-19)33-27-31-15-22(29)25(34-27)20-12-21(28)26-23(13-20)37(17(2)3)18(4)32-26/h6-7,12-15,17H,5,8-11,16H2,1-4H3,(H,30,31,33,34)
Chemical Name
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine
Synonyms
Abemaciclib; LY2835219; LY-2835219; LY 2835219; Abemaciclib methanesulfonate; Verzenio; LY2835219 free base; LY-2835219; UNII-60UAB198HK; Verzenios; LY2835219 methanesulfonate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: >10 mM
Water: N/A
Ethanol: N/A
Solubility (In Vivo)
Solubility in Formulation 1: 3.33 mg/mL (6.57 mM) in 0.5% HEC (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.

Solubility in Formulation 2: 5% DMSO+40% PEG 300+5%Tween80+ 50%ddH2O: 0.2mg/ml

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9740 mL 9.8699 mL 19.7398 mL
5 mM 0.3948 mL 1.9740 mL 3.9480 mL
10 mM 0.1974 mL 0.9870 mL 1.9740 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Clinical Trial Information
Stereotactic Radiation & Abemaciclib in the Management of HR+/HER2- Breast Cancer Brain Metastases
CTID: NCT04923542
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-29
Evaluation of Abemaciclib and Radiation Therapy Before Surgery for the Treatment of High-Risk Adipocytic Retroperitoneal Sarcoma
CTID: NCT06025747
Phase: Phase 1    Status: Recruiting
Date: 2024-11-27
A Study of Abemaciclib (LY2835219) in Women With HR+, HER2+ Locally Advanced or Metastatic Breast Cancer
CTID: NCT02675231
Phase: Phase 2    Status: Completed
Date: 2024-11-26
Abemaciclib in Patients With HIV-associated and HIV-negative Kaposi Sarcoma
CTID: NCT04941274
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25
Abemaciclib Neuropharmacokinetics of Diffuse Midline Glioma Using Intratumoral Microdialysis
CTID: NCT05413304
Phase: Phase 1    Status: Recruiting
Date: 2024-11-25
View More

Cyclin-Dependent Kinase (CDK)4/6 Inhibitor Abemaciclib for Neurofibromatosis Type I (NF1) Related Atypical Neurofibromas
CTID: NCT04750928
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-25


A Study Comparing Abemaciclib Plus Temozolomide to Temozolomide Monotherapy in Children and Young Adults With High-grade Glioma Following Radiotherapy
CTID: NCT06413706
Phase: Phase 2    Status: Recruiting
Date: 2024-11-22
Study of Abemaciclib and Elacestrant in Patients With Brain Metastasis Due to ER+/HER-2- Breast Cancer
CTID: NCT05386108
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-21
A Study of Abemaciclib and Radiation Therapy in People With Metastatic Breast Cancer
CTID: NCT06678269
Phase: Phase 1    Status: Recruiting
Date: 2024-11-21
TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer (Sub-Study A)
CTID: NCT05548127
Phase: Phase 1/Phase 2    Status: Active, not recruiting
Date: 2024-11-20
Saruparib (AZD5305) Plus Camizestrant Compared With CDK4/6 Inhibitor Plus Endocrine Therapy or Plus Camizestrant in HR-Positive, HER2-Negative (IHC 0, 1+, 2+/ ISH Non-amplified), BRCA1, BRCA2, or PALB2m Advanced Breast Cancer
CTID: NCT06380751
Phase: Phase 3    Status: Recruiting
Date: 2024-11-19
Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Patients With Metastatic Breast Cancer
CTID: NCT05563220
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-18
Abemaciclib in Patients with Oligodendroglioma
CTID: NCT03969706
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-18
A Study Evaluating the Efficacy and Safety of Adjuvant Giredestrant Compared With Physician's Choice of Adjuvant Endocrine Monotherapy in Participants With Estrogen Receptor-Positive, HER2-Negative Early Breast Cancer (lidERA Breast Cancer)
CTID: NCT04961996
Phase: Phase 3    Status: Recruiting
Date: 2024-11-18
A Study to Evaluate Efficacy and Safety of Giredestrant Compared With Fulvestrant (Plus a CDK4/6 Inhibitor), in Participants With ER-Positive, HER2-Negative Advanced Breast Cancer Resistant to Adjuvant Endocrine Therapy (pionERA Breast Cancer)
CTID: NCT06065748
Phase: Phase 3    Status: Recruiting
Date: 2024-11-15
A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer
CTID: NCT03424005
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-13
Named Patient Use Program to Provide Abemaciclib (LY2835219) for the Treatment of Metastatic Breast Cancer
CTID: NCT03763604
Phase:    Status: Available
Date: 2024-11-12
TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer
CTID: NCT02693535
Phase: Phase 2    Status: Recruiting
Date: 2024-11-12
Capivasertib + CDK4/6i + Fulvestrant for Advanced/Metastatic HR+/HER2- Breast Cancer (CAPItello-292)
CTID: NCT04862663
Phase: Phase 3    Status: Recruiting
Date: 2024-11-08
TRADE: Dose Escalation Tolerability of Abemaciclib in HR+ HER2- Early Stage Breast Cancer
CTID: NCT06001762
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-07
RESOLVE: Abemaciclib + Letrozole +/- Metformin or Zotatifin in Endometrial or Low-Grade Serous Ovarian Cancer
CTID: NCT03675893
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-07
Abemaciclib for Patients With Retinoblastoma-Positive, Triple Negative Metastatic Breast Cancer
CTID: NCT03130439
Phase: Phase 2    Status: Terminated
Date: 2024-11-06
A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer
CTID: NCT04802759
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-06
An Adjuvant Endocrine-based Therapy Study of Camizestrant (AZD9833) in ER+/HER2- Early Breast Cancer (CAMBRIA-2)
CTID: NCT05952557
Phase: Phase 3    Status: Recruiting
Date: 2024-11-05
ALPINE: Maintenance Letrozole/Abemaciclib Vs Pembrolizumab
CTID: NCT06366347
Phase: Phase 2    Status: Recruiting
Date: 2024-10-31
Vismodegib, FAK Inhibitor GSK2256098, Capivasertib, and Abemaciclib in Treating Patients With Progressive Meningiomas
CTID: NCT02523014
Phase: Phase 2    Status: Recruiting
Date: 2024-10-28
Genetic Testing in Guiding Treatment for Patients With Brain Metastases
CTID: NCT03994796
Phase: Phase 2    Status: Recruiting
Date: 2024-10-26
LY3214996 and Cetuximab Alone or in Combination With Abemaciclib for the Treatment of Unresectable or Metastatic Colorectal Cancer
CTID: NCT04616183
Phase: Phase 1/Phase 2    Status: Active, not recruiting
Date: 2024-10-26
A Study of LOXO-783 in Patients With Breast Cancer/Other Solid Tumors
CTID: NCT05307705
Phase: Phase 1    Status: Active, not recruiting
Date: 2024-10-26
Testing the Addition of an Anti-Cancer Drug, Abemaciclib, to the Usual Chemotherapy Treatment (5-Fluorouracil) for Metastatic, Refractory Colorectal Cancer
CTID: NCT06654037
Phase: Phase 1    Status: Not yet recruiting
Date: 2024-10-23
I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer
CTID: NCT01042379
Phase: Phase 2    Status: Recruiting
Date: 2024-10-22
Abemaciclib Dose Escalation to Maintain Intensity (ADE-MI)
CTID: NCT06169371
Phase: Phase 4    Status: Recruiting
Date: 2024-10-22
A Study of Abemaciclib (LY2835219) in Participants With Previously Treated KRAS Mutated Lung Cancer
CTID: NCT02152631
Phase: Phase 3    Status: Active, not recruiting
Date: 2024-10-21
A Study of Multiple Immunotherapy-Based Treatment Combinations in Hormone Receptor (HR)-Positive Human Epidermal Growth Factor Receptor 2 (HER2)-Negative Breast Cancer
CTID: NCT03280563
Phase: Phase 1/Phase 2    Status: Completed
Date: 2024-10-21
A Study of Imlunestrant, Investigator's Choice of Endocrine Therapy, and Imlunestrant Plus Abemaciclib in Participants With ER+, HER2- Advanced Breast Cancer
CTID: NCT04975308
Phase: Phase 3    Status: Active, not recruiting
Date: 2024-10-18
A Study of Abiraterone Acetate Plus Prednisone With or Without Abemaciclib (LY2835219) in Participants With Prostate Cancer
CTID: NCT03706365
Phase: Phase 2/Phase 3    Status: Active, not recruiting
Date: 2024-10-18
Abemaciclib and Niraparib Before Surgery for the Treatment of Hormone Receptor Positive HER2 Negative Breast Cancer
CTID: NCT04481113
Phase: Phase 1    Status: Active, not recruiting
Date: 2024-10-17
A Study of Abemaciclib (LY2835219) in Participants With Breast Cancer
CTID: NCT02763566
Phase: Phase 3    Status: Active, not recruiting
Date: 2024-10-16
Testing the Addition of an Anti-cancer Drug, Abemaciclib, to the Usual Chemotherapy Treatment (Gemcitabine) for Soft Tissue Sarcoma
CTID: NCT06498648
Phase: Phase 1/Phase 2    Status: Not yet recruiting
Date: 2024-10-15
CAMPFIRE: A Study of Abemaciclib (LY2835219) in Participants With Ewing's Sarcoma
CTID: NCT05440786
Phase: Phase 2    Status: Recruiting
Date: 2024-10-15
Testing the Safety and Efficacy of the Combination of Two Anti-cancer Drugs, ZEN003694 and Abemaciclib, for Adult and Pediatric Patients (12-17 Years) With Metastatic or Unresectable NUT Carcinoma, Breast Cancer and Other Solid Tumors
CTID: NCT05372640
Phase: Phase 1    Status: Recruiting
Date: 2024-10-09
A Study of Nonsteroidal Aromatase Inhibitors Plus Abemaciclib (LY2835219) in Postmenopausal Women With Breast Cancer
CTID: NCT02246621
Phase: Phase 3    Status: Active, not recruiting
Date: 2024-10-08
A Precision Medicine Approach (SMMART-ACT) for the Treatment of Patients With Advanced, Recurrent Sarcoma, Prostate, Breast, Ovarian or Pancreatic Cancer
CTID: NCT06630325
Phase: Phase 2    Status: Not yet recruiting
Date: 2024-10-08
A Study to Evaluate Abemaciclib in Advanced Biliary Tract Carcinoma
CTID: NCT04003896
Phase: Phase 2    Status: Terminated
Date: 2024-10-08
ETHAN - ET for Male BC
CTID: NCT05501704
Phase: Phase 2    Status: Recruiting
Date: 2024-10-03
A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors
CTID: NCT06188520
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-10-03
CB-103 With Either Lenvatinib or Abemaciclib in Patients With NOTCH ACC
CTID: NCT05774899
Phase: Phase 1/Phase 2    Status: Active, not recruiting
Date: 2024-10-02
Endocrine Therapy With or Without Abemaciclib (LY2835219) Following Surgery in Participants With Breast Cancer
CTID: NCT03155997
Phase: Phase 3    Status: Active, not recruiting
Date: 2024-10-01
Sequential Therapies Modeled on Evolutionary Dynamics for Breast Cancer
CTID: NCT06409390
PhaseEarly P
The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs to determine the Efficacy in Treatment of Advanced Cancers with a Known Molecular Profile
CTID: null
Phase: Phase 2    Status: Trial now transitioned
Date: 2021-10-06
SERENA-6: A Phase III, Double-blind, Randomised Study to Assess Switching to AZD9833 (a Next Generation, Oral SERD) + CDK4/6 Inhibitor (Palbociclib or Abemaciclib) vs Continuing Aromatase Inhibitor (Letrozole or Anastrozole) + CDK4/6 Inhibitor in HR+/HER2- MBC Patients with Detectable ESR1 Mutation Without Disease Progression During 1L Treatment with Aromatase Inhibitor + CDK4/6 Inhibitor
CTID: null
Phase: Phase 3    Status: Trial now transitioned, Ongoing
Date: 2021-07-28
A Phase Ib/III Randomised Study of Capivasertib plus CDK4/6i and Fulvestrant versus Placebo plus CDK4/6 Inhibitors and Fulvestrant in Hormone Receptor-Positive and Human Epidermal Growth Factor Receptor 2-Negative Locally Advanced, Unresectable or Metastatic Breast Cancer
CTID: null
Phase: Phase 1, Phase 3    Status: Trial now transitioned, Ongoing
Date: 2021-07-14
randomized, 2-arm, open-label, phase II study of abemaciclib combined with
CTID: null
Phase: Phase 2    Status: Trial now transitioned, Ongoing
Date: 2021-06-23
eMonarcHER: A Randomized, Double Blind, Placebo-Controlled Phase 3 Study of Abemaciclib plus Standard Adjuvant Endocrine Therapy in Participants with High-Risk, Node-Positive, HR+, HER2+ Early Breast Cancer Who Have Completed Adjuvant HER2-Targeted Therapy
CTID: null
Phase: Phase 3    Status: Temporarily Halted, Prematurely Ended, Completed
Date: 2021-04-26
Randomized, Non-comparative Neoadjuvant Phase II Study in Patients with ER+/HER2- Breast Cancer >= 2 cm with Safety Run-in, Assessing Nivolumab + Abemaciclib or Palbociclib + Anastrozole
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2020-12-10
A Phase 1b/2 Study of Abemaciclib in Combination with Irinotecan and Temozolomide (Part A) and Abemaciclib in Combination with Temozolomide (Part B) in
CTID: null
Phase: Phase 1    Status: Trial now transitioned, Completed
Date: 2020-10-03
EMBER: A Phase 1a/1b Study of LY3484356 Administered as Monotherapy and in Combination with Anticancer Therapies for Patients with ER+ Locally Advanced or Metastatic Breast Cancer and Other Select Non-Breast Cancers
CTID: null
Phase: Phase 1, Phase 2    Status: Trial now transitioned
Date: 2020-09-08
CYCLONE 1: A Phase 2 Study of Abemaciclib in Metastatic Castration-Resistant Prostate Cancer Patients Previously Treated with a Novel Hormonal Agent and Taxane-based Chemotherapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2020-08-17
A randomized, controlled, open-label, phase-III trial on Adjuvant Dynamic marker - Adjusted Personalized Therapy comparing abemaciclib combined with standard adjuvant endocrine therapy versus standard adjuvant endocrine therapy in (clinical or genomic) high risk, HR+/HER2- early breast cancer.
CTID: null
Phase: Phase 3    Status: Trial now transitioned
Date: 2020-07-09
PreOperative Endocrine Therapy for Individualised Care with Abemaciclib
CTID: null
Phase: Phase 3    Status: GB - no longer in EU/EEA
Date: 2020-07-06
Phase II, randomized, open-label, international, multicenter study to compare efficacy of standard chemotherapy vs. letrozole plus abemaciclib as neoadjuvant therapy in HR-positive/HER2-negative high/intermediate risk breast cancer patients. “CARABELA Study”
CTID: null
Phase: Phase 2    Status: Ongoing
Date: 2020-06-15
Open-label, randomized, multicenter, phase III study, comparing standard chemotherapy to standard combination of endocrine therapy with Abemaciclib as initial Metastatic treatment among patients with visceral metastasis of ER+ HER2- BREast cancer, high burden disease
CTID: null
Phase: Phase 3    Status: Trial now transitioned
Date: 2020-01-30
A Phase 2, open label, multicenter, single arm trial evaluating the activity and safety of Abemaciclib + Aromatase Inhibitors (AIs) after 1st-line treatment with High-Dose Fulvestrant in Hormone-Receptor-Positive (HR+), Human-Epidermal-Growth-factor-negative (HER2-) advanced breast cancer patients. The HERMIONE-7 trial
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2019-10-31
A Phase 2, Randomized, Double-blind, Placebo-Controlled Study of Abiraterone Acetate Plus Prednisone with or without Abemaciclib in Patients with Metastatic Castration-Resistant Prostate Cancer
CTID: null
Phase: Phase 2    Status: Ongoing, Restarted, Trial now transitioned, Completed
Date: 2019-01-02
Multiorgan Metabolic imaging response assessment of Abemaciclib: the MiMe-A trial
CTID: null
Phase: Phase 2    Status: Completed
Date: 2018-11-14
An Open-Label, Randomized Phase 2 Study of the Impact of Food on Tolerability when Receiving Abemaciclib for Patients with Previously Treated Hormone Receptor-Positive, HER2-Negative, Metastatic Breast Cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2018-10-31
Mesothelioma Stratified Therapy (MiST):
CTID: null
Phase: Phase 2    Status: GB - no longer in EU/EEA
Date: 2018-07-05
An Phase II trial aiming to evaluate the clinical interest of ABEMACICLIB monotherapy in patients with locally advanced/metastatic head and neck cancer after failure of platinum and cetuximab or anti-EGFR-based therapy and harboring an homozygous deletion of CDKN2A, and/or an amplification of CCND1 and/or of CDK6
CTID: null
Phase: Phase 2    Status: Completed
Date: 2017-11-06
Selecting the Optimal position of CDK4/6 Inhibitors in HR+ Advanced breast cancer: the SONIA trial
CTID: null
Phase: Phase 3    Status: Ongoing
Date: 2017-09-29
A Randomized, Open-Label, Phase 3 Study of Abemaciclib Combined with Standard Adjuvant Endocrine Therapy versus Standard Adjuvant Endocrine Therapy Alone in Patients with High-Risk, Node-Positive, Early-Stage, Hormone Receptor-Positive, Human Epidermal Receptor 2-Negative, Breast Cancer
CTID: null
Phase: Phase 3    Status: Trial now transitioned, GB - no longer in EU/EEA, Ongoing
Date: 2017-08-14
An Adaptive, Open-Label, Randomized Phase 2 Study of Abemaciclib as a Monotherapy and in Combination with Other Agents Versus Choice of Standard of Care (Gemcitabine or Capecitabine) in Patients with Previously Treated Metastatic Pancreatic Ductal Adenocarcinoma
CTID: null
Phase: Phase 2    Status: Completed, Prematurely Ended
Date: 2017-01-17
A Randomized, Open-Label, Phase 2 Study of Abemaciclib plus Tamoxifen or Abemaciclib Alone, in Women with Previously Treated Hormone Receptor-Positive, HER2-Negative, Metastatic Breast Cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2016-07-21
Protocol I3Y-MC-JPCE
CTID: null
Phase: Phase 1, Phase 2    Status: Ongoing, Trial now transitioned, Completed
Date: 2016-06-15
monarcHER: A Phase 2, Randomized, Multicenter, 3-Arm, Open-Label Study to Compare the Efficacy of Abemaciclib plus Trastuzumab with or without Fulvestrant to Standard-of-Care Chemotherapy of Physician’s Choice plus Trastuzumab in Women with HR+, HER2+ Locally Advanced or Metastatic Breast Cancer
CTID: null
Phase: Phase 2    Status: GB - no longer in EU/EEA, Completed
Date: 2016-01-29
A Randomized Phase 2 Study of Abemaciclib (LY2835219) versus Docetaxel in Patients with Stage IV Squamous Non-Small Cell Lung Cancer Previously Treated with Platinum-based Chemotherapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-09-18
neoMONARCH: A Phase 2 Neoadjuvant Trial Comparing the Biological Effects of 2 Weeks of Abemaciclib (LY2835219) in Combination with Anastrozole to those of Abemaciclib Monotherapy and Anastrozole Monotherapy and Evaluating the Clinical Activity and Safety of a Subsequent 14 Weeks of Therapy with Abemaciclib in Combination with Anastrozole in Postmenopausal Women with Hormone Receptor Positive, HER2 Negative Breast Cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-07-24
A Single-Arm, Multicenter, Phase 1b Study with an Expansion Cohort to Evaluate Safety and Efficacy of Necitumumab in Combination with Abemaciclib in Treatment of Patients with Stage IV Non-Small Cell Lung Cancer (NSCLC)
CTID: null
Phase: Phase 1, Phase 2    Status: Completed
Date: 2015-04-21
A Phase 2 Study of Abemaciclib in Patients with Brain Metastases Secondary to Hormone Receptor Positive Breast Cancer, Non-small Cell Lung Cancer, or Melanoma
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-03-10
A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Study of Nonsteroidal Aromatase Inhibitors (Anastrozole or Letrozole) Plus LY2835219, a CDK4/6 Inhibitor, or Placebo in Postmenopausal Women With Hormone Receptor-Positive, HER2-Negative Locoregionally Recurrent or Metastatic Breast Cancer With No Prior Systemic Therapy in This Disease Setting
CTID: null
Phase: Phase 3    Status: Ongoing, GB - no longer in EU/EEA, Completed
Date: 2014-11-24
A Randomized Phase 3 Study of LY2835219 plus Best Supportive Care versus Erlotinib plus Best Supportive Care in Patients with Stage IV NSCLC with a Detectable KRAS Mutation Who Have Progressed After Platinum Based Chemotherapy
CTID: null
Phase: Phase 3    Status: Ongoing, Completed
Date: 2014-09-17
A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Study of Fulvestrant with or without LY2835219, a CDK4/6 Inhibitor, for Women with Hormone Receptor Positive, HER2 Negative Locally Advanced or Metastatic Breast Cancer
CTID: null
Phase: Phase 3    Status: Completed, Trial now transitioned, Ongoing
Date: 2014-07-09
A Phase 2 Study of LY2835219 for Patients with Previously Treated Hormone Receptor Positive, HER2 Negative Metastatic Breast Cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2014-05-16
A Randomized, Open-Label, Phase 2 Study Evaluating Abemaciclib in Combination with Irinotecan and Temozolomide in Participants with Relapsed or Refractory Ewing's Sarcoma
CTID: null
Phase: Phase 2    Status: Trial now transitioned, Ongoing
Date:
Phase II study of nivolumab + abemaciclib + endocrine therapy in patients with HR-positive HER2-negative metastatic breast cancer(WJOG11418B Investigator-Initiated Clinical Trial)
CTID: jRCT2080224706
Phase:    Status: terminated
Date: 2019-06-01
None
CTID: jRCT2080224656
Phase:    Status: completed
Date: 2019-04-22
I3Y-MC-JPCF
CTID: jRCT2080223612
Phase:    Status: completed
Date: 2017-08-07
Phase I study of xentuzumab and abemaciclib
CTID: jRCT2080223555
Phase:    Status: completed
Date: 2017-06-12
None
CTID: jRCT2080222563
Phase:    Status: completed
Date: 2014-07-23

Biological Data
  • Abemaciclib (LY2835219)


    Effects of LY2835219 on RB pathway and intracellular signaling.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    Combined effect of LY2835219 and mTOR inhibitorsin vitro.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    LY2835219 and mTOR inhibitor combination in HNSCC xenograft tumor model.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    Antitumor activity of LY2835219 in HNSCC xenograft tumor model.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    Effects of CDK4/6 inhibitor LY2835219 on cell growth in HNSCC.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    Effects of LY2835219 on cell proliferation and cell cycle in HNSCC.2016 Mar 22;7(12):14803-13.

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