Piclib — Palbociclib 125 mg, 21 Capsules

Piclib is supplied in the form of hard gelatin capsules for oral administration. Each box contains 21 capsules (intended for one 28-day treatment cycle):

• Active Ingredient: Palbociclib — 125 mg per capsule.
• Excipients: Microcrystalline cellulose, lactose monohydrate, sodium starch glycolate, colloidal silicon dioxide, magnesium stearate.
• Capsule Shell: Gelatin, titanium dioxide, iron oxide red/yellow colorants.

Pharmacodynamics: Palbociclib is a selective, reversible inhibitor of cyclin-dependent kinases CDK4 and CDK6. These enzymes regulate the cell cycle by driving transition from G1 to S phase. In estrogen receptor-positive (ER+) breast cancer cells, hyperactivation of CDK4/6 leads to uncontrolled cell proliferation. By inhibiting these kinases, Piclib arrests cell cycle progression and suppresses tumor growth.

Pharmacokinetics: Peak plasma concentration (Cmax) of palbociclib is achieved between 6 and 12 hours after oral administration. Administration with food increases absorption and reduces inter-individual variability. Plasma protein binding is approximately 85%. It is extensively metabolized in the liver mainly via CYP3A4 and aldoreductase enzymes. The mean elimination half-life (T1/2) is about 29 hours. Excretion occurs primarily via feces (74%) and urine (17%).

Piclib (Palbociclib) 125 mg is indicated for the treatment of adult patients with advanced breast cancer:

• 🔹 Treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) locally advanced or metastatic breast cancer.
• 🔹 In combination with an aromatase inhibitor (e.g., letrozole, anastrozole) as initial endocrine-based therapy in postmenopausal women.
• 🔹 In combination with fulvestrant in women who have received prior endocrine therapy.

Piclib must be administered under the supervision of a qualified oncologist:

• 💊 Recommended Dosage: The starting dose is 125 mg (1 capsule) taken orally once daily.
• 🗓️ Treatment Schedule: Taken daily for 21 consecutive days followed by 7 days off treatment (forming a complete 28-day cycle).
• 🍽️ Administration: Capsules should be swallowed whole with food (preferably at the same time each day) and water. Do not chew, open, or crush capsules.
• ⚠️ Dose Modification: Depending on individual safety and hematologic toxicity (e.g., severe neutropenia), dose reduction to 100 mg or 75 mg daily may be required.

The use of Piclib is contraindicated in the following cases:

• ❌ Hypersensitivity to palbociclib or any excipients in the formulation.
• ❌ Pregnancy and breastfeeding period.
• ❌ Severe renal or hepatic impairment (due to limited clinical data).
• ❌ Pediatric patients under 18 years of age (safety and efficacy not established).
• ❌ Concomitant use with strong CYP3A4 inhibitors or inducers, as well as St. John's Wort preparations.

Key drug interactions with Piclib include:

• ⚠️ Strong CYP3A4 Inhibitors: Concomitant use with strong inhibitors (e.g., ketoconazole, clarithromycin, grapefruit juice) increases palbociclib exposure and toxicity risk; co-administration should be avoided.
• ⚠️ Strong CYP3A4 Inducers: Strong inducers (rifampin, phenytoin, carbamazepine, St. John's Wort) significantly decrease palbociclib plasma concentration and clinical efficacy.
• ⚠️ CYP3A4 Substrates: Palbociclib may increase plasma exposure of drugs with narrow therapeutic index metabolized by CYP3A4.

The use of Piclib during pregnancy and breastfeeding is subject to strict warnings:

• 🤰 Pregnancy: Contraindicated. Palbociclib causes fetal toxicity and malformations.
• 🚫 Contraception: Females of childbearing potential must use effective contraception during treatment and for at least 3 weeks after the last dose. Males must use contraception for 14 weeks post-treatment.
• 🤱 Lactation: It is unknown whether palbociclib is excreted in human milk. Breastfeeding must be discontinued during treatment.

Treatment with Piclib may cause side effects requiring regular clinical monitoring:

• 🩸 Hematologic: Neutropenia, leukopenia, anemia, thrombocytopenia (most common reactions; require routine blood counts).
• 🦠 Infections: Increased susceptibility to upper respiratory tract infections, stomatitis.
• 🤢 Gastrointestinal: Nausea, diarrhea, vomiting, decreased appetite, dysgeusia.
• 💆 General: Fatigue, asthenia, alopecia (thinning hair), rash, dry skin.
• 🧪 Laboratory: Elevated ALT and AST liver enzyme levels.

Overdose Symptoms: Exacerbation of toxic reactions, particularly severe neutropenia, thrombocytopenia, and high risk of infections.

Management: There is no specific antidote for palbociclib. In case of overdose, discontinue medication, provide supportive care, and closely monitor hematologic parameters.

Storage instructions for Piclib 125 mg:

• 🌡️ Temperature: Store below 30 °C.
• 💧 Moisture & Light Protection: Store in the original package to protect from light and moisture.
• 👶 Child Safety: Keep out of reach of children.
• ⏳ Shelf Life: Observe expiration date printed on the pack.

Hetero incorporates several packaging protection features to ensure authenticity and protect against counterfeiting:

• 🛡️ HETERO Security Hologram: A tamper-evident holographic seal featuring the "HETERO" logo is affixed over the top box closure flap.
• 🔍 Batch Details: The side panel displays laser-printed or stamped Batch Number (Batch No.), Manufacturing Date (Mfg. Date), Expiry Date (Exp. Date), and Maximum Retail Price (M.R.P.).
• 📦 Brand Identity: Packaging features the official ONCOLOGY Hetero logo and a unique scannable barcode on the box.