Palbokin 125 capsule: Each capsule contains Palbociclib INN 125 mg.

Palbociclib is an inhibitor of cyclin-dependent kinases (CDK) 4 and 6. Cyclin D1 and CDK4/6
are downstream of signaling pathways which lead to cellular proliferation. In vitro, Palbociclib
reduced cellular proliferation of estrogen receptor (ER)-positive breast cancer cell lines by
blocking progression of the cell from G1 into S phase of the cell cycle. Treatment of breast
cancer cell lines with the combination of Palbociclib and antiestrogens leads to decreased
retinoblastoma (Rb) protein phosphorylation resulting in reduced E2F expression and
signaling, and increased growth arrest compared to treatment with each drug alone. In vitro
treatment of ER-positive breast cancer cell lines with the combination of Palbociclib and
antiestrogens led to increased cell senescence compared to each drug alone, which was
sustained for up to 6 days following Palbociclib removal and was greater if antiestrogen
treatment was continued. In vivo studies using a patient-derived ER-positive breast cancer
xenograft model demonstrated that the combination of Palbociclib and letrozole increased the
inhibition of Rb phosphorylation, downstream signaling, and tumor growth compared to each
drug alone. Human bone marrow mononuclear cells treated with Palbociclib in the presence or
absence of an anti-estrogen in vitro did not become senescent and resumed proliferation
following Palbociclib withdrawal.

Palbociclib is indicated for the treatment of HR-positive, HER2-negative advanced or
metastatic breast cancer in combination with:
• an aromatase inhibitor as initial endocrine based therapy in postmenopausal women; or
• fulvestrant in women with disease progression following endocrine therapy

The recommended dose of Palbociclib is a 125 mg capsule taken orally once daily for 21
consecutive days followed by 7 days off treatment to comprise a complete cycle of 28 days.
Palbociclib should be taken with food. Administer the recommended dose of an aromatase
inhibitor when given with Palbociclib. Please refer to the Full Prescribing Information for the
aromatase inhibitor being used. When given with Palbociclib, the recommended dose of
fulvestrant is 500 mg administered on Days 1, 15, 29, and once monthly thereafter. Please
refer to the Full Prescribing Information of fulvestrant. Pre/perimenopausal women treated with
the combination Palbociclib plus fulvestrant therapy should be treated with luteinizing
hormone-releasing hormone (LHRH) agonists according to current clinical practice standards.

Neutropenia: Complete blood count should be monitored prior to start of Palbociclib therapy 
and at the beginning of each cycle, as well as on Day 15 of the first 2 cycles, and as clinically
indicated.
• Embryo-Fetal Toxicity: Palbociclib can cause fetal harm. Patients should be advised about
potential risk to the fetus and to use effective contraception.
Adverse Reactions:
Most common adverse reactions (incidence ≥10%) were neutropenia, infections, leukopenia,
fatigue, nausea, stomatitis, anemia, alopecia, diarrhea, thrombocytopenia, rash, vomiting,
decreased appetite, asthenia, and pyrexia. 

None

Based on findings from animal studies and its mechanism of action, Palbociclib can cause fetal
harm when administered to a pregnant woman. There are no available data in pregnant women
to inform the drug-associated risk.

Palbokin 125 capsule: Each HDPE container of Palbokin 125 contains 30 capsules, a silica
gel desiccant and polyester coil with a child resistant closure. 

CYP3A Inhibitors: Avoid concurrent use of Palbociclib with strong CYP3A inhibitors. If the
strong inhibitor cannot be avoided, reduce the Palbociclib dose.
CYP3A Inducers: Avoid concurrent use of Palbociclib with strong CYP3A inducers. 

There is no information regarding the presence of Palbociclib in human milk, its effects on milk
production, or the breastfed infant. Because of the potential for serious adverse reactions in
breastfed infants from Palbociclib, advise a lactating woman not to breastfeed during treatment
with Palbociclib and for 3 weeks after the last dose.

There is no known antidote for Palbociclib. The treatment of overdose of Palbociclib should
consist of general supportive measures.

The safety and effectiveness of Palbociclib in pediatric patients have not been established.

Do not Store above 30° C. Protect from light. Keep out of the reach of children.