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CDK46 Inhibitors for Treatment of Advanced Breast Cancer .pdf

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Huateng Pharm


CDK4/6 Inhibitors for Treatment of
Advanced Breast Cancer
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. In 2018, it is estimated that
627,000 women died from breast cancer – that is approximately 15%
of all cancer deaths among women. While breast cancer rates are
higher among women in more developed regions, rates are increasing
in nearly every region globally.
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
1. Verzenio (Abemaciclib)
According to the approval time from near to far, let's look at Verzenio
first. Verzenio is a selective CDK4 and CDK6 inhibitor with IC50 values
of 2 nM and 10 nM for CDK4 and CDK6 inhibitory activity,

The FDA granted Verzenio "breakthrough therapy" status in 2015,
and then received Eli Lilly's New Drug Application on May 5, 2017,
followed by Verzenio priority review status on July 10, 2017. There
are two approved Verzenio therapies. One is combined with
fulvestrant to treat female patients with advanced HR-positive and

Huateng Pharm


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.
Common side effects that Verzenio may cause include diarrhea,
neutropenia, nausea, abdominal pain, infection, fatigue, decreased
red blood cell levels (anemia), loss of appetite, vomiting, headache.
Serious side effects include diarrhea, neutropenia, liver Examination
of blood and coagulation (deep vein thrombosis / pulmonary
embolism). In addition, Verzenio may cause harm to developing
fetuses and is not suitable for pregnant women.
2. Kisqali (Ribociclib)
Kisqali is the second FDA-approved oral CDK4 / 6 inhibitor with IC50
values of 10 nM and 39 nM for CDK4 and CDK6 inhibitory activity,

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. Kisqali has achieved breakthrough therapy
and priority review certification before being approved.
Common side effects seen in patients include neutropenia, nausea,

Huateng Pharm


fatigue, diarrhea, leukopenia, hair loss, vomiting, constipation,
headache and back pain.
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.

Although Pfizer's development of Ibrance has been bumpy. But finally,
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.
Common side effects seen in patients include Nausea, vomiting, loss
of appetite, diarrhea, tiredness, weakness, hair loss, mouth sores, or
numbness/tingling of arms/legs.
Huateng Pharma, a professional manufacturer of pharmaceutical API
and intermediates, provides Palbociclib and Ribociclib key
intermediates with high purity.
Palbociclib Intermediates: CAS NO. 571189-16-7
Ribociclib Intermediates: CAS No.: 733039-20-8

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