CDK4 inhibitors(Cyclin-dependent kinase 4 inhibitors), CDK6 inhibitors(Cyclin-dependent kinase 6 inhibitors), ERs antagonists(Estrogen receptors antagonists)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal Diseases

Active Indication

Hormone receptor positive HER2 negative breast cancer

Inactive Indication-

Originator Organization

Novartis Pharma AG

Active Organization

Novartis Pharmaceuticals Corp.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (04 May 2017),

Hormone receptor positive HER2 negative breast cancer

RegulationBreakthrough Therapy (US)

Structure

Molecular FormulaC17H11N5

InChIKeyHPJKCIUCZWXJDR-UHFFFAOYSA-N

CAS Registry112809-51-5

View All Structures (2)

Clinical Trials associated with Letrozole/Ribociclib Succinate

NCT05163106 / RecruitingPhase 2

Presurgical Treatment With Ribociclib and Letrozole in Patients With Locally Advanced Breast Cancer: the NEOLETRIB Study.

Patients with locally advanced (stage III) breast cancer (LABC) are characterized by a significantly worse prognosis compared to patients with primarily operable breast cancer. While neoadjuvant chemotherapy has been the first choice in this situation for several decades, recent evidence suggests that some patients may experience an extraordinary effect from neoadjuvant endocrine treatments involving aromatase inhibitors as monotherapy or in modern drug combinations.Selected LABC patients admitted for treatment will be offered combination therapy including letrozole and ribociclib. The overall goal of the project is to improve understanding of tumor responses and resistance in patients suffering from ER-positive/HER-2 negative locally advanced breast cancer, focusing on the role of the immune system including the gut microbiome.

Start Date01 Dec 2022

Sponsor / Collaborator

Akershus Universitetssykehus HF

[+2]

NCT03283384 / Active, not recruitingPhase 2IIT

Tailoring NEOadjuvant Therapy in Hormone Receptor Positive, HER2 Negative, Luminal Breast Cancer.

The aim of this prospective, randomized, multicenter, open-label, phase II study is to test if chemotherapy can be replaced by the combination of ribociclib plus letrozole as a neo-adjuvant therapy for patients with non-metastatic primary luminal breast cancer.

Start Date15 Jun 2019

Sponsor / Collaborator

Novartis AG

[+1]

100 Clinical Results associated with Letrozole/Ribociclib Succinate

100 Translational Medicine associated with Letrozole/Ribociclib Succinate

100 Patents (Medical) associated with Letrozole/Ribociclib Succinate

Literatures (Medical) associated with Letrozole/Ribociclib Succinate

01 Sep 2023·Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners

Toxic hepatitis in metastatic breast cancer patient using ribociclib and denosumab.

Article

Author: Aktürk Esen, Selin ; Köş, Fahriye Tuğba ; Bayram, Doğan ; Uçar, Gökhan

INTRODUCTION:

Hepatotoxicity is observed due to cyclin-dependent kinase (CDK4/6) inhibitors used to treat hormone receptor-positive metastatic breast cancer. However, it should not be ignored that denosumab may be hepatotoxic, although it is rare.

CASE REPORT:

A 73-year-old female patient with breast cancer with axillary lymph node, adrenal gland and bone metastases was started on ribociclib letrozole and denosumab treatment. Ribociclib treatment was discontinued due to grade 4 hepatotoxicity during treatment, but liver function tests did not decrease. After discontinuation of denosumab treatment, alanine aminotransferase and aspartate aminotransferase values regressed to baseline values.

MANAGEMENT AND OUTCOME:

Despite the discontinuation of ribociclib treatment, other causes of liver toxicity were investigated due to persistence of hepatic transaminases and elevation. Autoimmune hepatitis markers were negative. Hepatobiliary USG did not reveal any pathological findings except hepatosteatosis. Liver biopsy was performed to determine the etiology. Pathology result was compatible with acute hepatocellular damage (in favor of toxic hepatitis). A decrease in liver values was detected after discontinuation of denosumab treatment.

DISCUSSION:

Although cases with improvement in liver enzymes have been reported after discontinuation of ribociclib, no improvement in hepatotoxicity was observed in our case. Since the liver biopsy was toxic hepatitis, it was thought that other drugs used by the patient might cause this toxicity, and a significant decrease was observed in liver values after discontinuation of denosumab. Denosumab-induced liver toxicity is very rare, and there are only a limited number of cases in the literature.

100 Deals associated with Letrozole/Ribociclib Succinate

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	L01XE	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hormone receptor positive HER2 negative breast cancer	US	Novartis Pharmaceuticals Corp.	04 May 2017

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03248427 (CORALLEEN, Pubmed \| Lancet Oncol) Manual	Phase 2	PIK3CA mutation/HR-positive/HER2-negative Breast Cancer Neoadjuvant HR positive \| HER2-negative	106	Ribociclib plus letrozole	lgxsiqljgt(qnqjyoarbi) = gvtdssbycv ahuqiqxinr (tzlrfwofvq, 32.5 ~ 61.7)	Positive	01 Jan 2020
				doxorubicin+cyclophosphamide+paclitaxel	lgxsiqljgt(qnqjyoarbi) = kodvckojvk ahuqiqxinr (tzlrfwofvq, 32.9 ~ 61.5)

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