Huateng Pharma Supplies Intermediates of CDK4/6 Inhibitors for Treatment of Advanced Breast Cancer

CHANGSHA, China - June 28, 2023 - PRLog -- Breast cancer is the most frequent cancer among women, impacting 2.1 million women each year, and also causes the greatest number of cancer-related deaths among women.

The majority of patients with metastatic breast cancer (MBC) have hormone receptor-positive HER2-negative disease. For this subgroup, endocrine therapy is the key therapeutic option. Recently, therapeutic options have been expanded by the introduction of the inhibitors of cyclin-dependent kinases 4/6 (CDK4/6i). Three compounds, palbociclib, ribociclib, and abemaciclib, have already been approved by the FDA for use together with endocrine therapy such as aromatase inhibitors (AIs) or fulvestrant; abemaciclib is also approved as a single agent. Now, let's make a comparison of CDK4/6 inhibitors.

1. Verzenio (Abemaciclib)

Verzenio is a selective CDK4 and CDK6 inhibitor with IC50 values ​​of 2 nM and 10 nM for CDK4 and CDK6 inhibitory activity, respectively.

There are two approved Verzenio therapies. One is combined with fulvestrant to treat female patients with advanced HR-positive and HER2-negative advanced metastatic breast cancer who have deteriorated after receiving endocrine therapy; the other is used as a monotherapy to treat adult patients with advanced metastatic breast cancer who were exacerbated after endocrine therapy and who were HR positive and HER2 negative before chemotherapy. Compared with other drugs of the same type, its characteristic is that it can be used as a monotherapy.

2. Kisqali (Ribociclib)

Kisqali is the second FDA-approved oral CDK4 / 6 inhibitor (https://us.huatengsci.com/news/show/1503.html) with IC50 values ​​of 10 nM and 39 nM for CDK4 and CDK6 inhibitory activity, respectively.

On March 13, 2017, Kisqali, a targeted anticancer drug developed by Novartis, was approved by the FDA. The combination of Kisqali and aromatase inhibitors are the first-line treatment for women with HR-positive and HER2-negative postmenopausal advanced metastatic breast cancer (https://us.huatengsci.com/news/show/1623.html). Kisqali has achieved breakthrough therapy and priority review certification before being approved.

3, Ibrance (Palbociclib)

Ibrance is an FDA-approved CDK4 / 6 inhibitor with IC50 values ​​of 11 nM and 16 nM for CDK4 and CDK6 inhibitory activity, respectively.

On February 3, 2015, the FDA accelerated the approval of Ibrance's marketing application, which is used in combination with letrozole to treat postmenopausal metastatic breast cancer patients with estrogen receptor (ER) positive and human epidermal growth factor receptor 2 (HER2) negative. Also prior to approval, Ibrance has achieved breakthrough therapy certification and priority review qualifications. Ibrance's successful launch is a milestone in the development of CDK inhibitors.

Huateng Pharma (https://us.huatengsci.com/product/175.html), a professional manufacturer of pharmaceutical API and intermediates (https://us.huatengsci.com/news/175.html), provides Palbociclib and Ribociclib key intermediates with high purity.

Palbociclib Intermediates: CAS NO. 571189-16-7, CAS No. 571188-59-5
Ribociclib Intermediates:  CAS No.: 733039-20-8, CAS No. 571188-59-5, ​CAS No. 52092-47-4