Airuikang (Dalpiciclib Isethionate) | Breast Cancer

Dalpiciclib Isethionate Application Scope

• Approved in China (Dec 31, 2021) in combination with fulvestrant for treatment of hormone receptor–positive (HR⁺), HER2-negative recurrent or metastatic breast cancer after progression on endocrine therapy

• Under clinical investigation in HR⁺/HER2⁻ early and advanced breast cancer, castration‑sensitive prostate cancer, HER2-positive breast cancer, malignant melanoma, ovarian, and other solid tumors

Dalpiciclib Isethionate Characteristics

• Ingredients:

  • Active: Dalpiciclib (cyclin-dependent kinase 4/6 inhibitor), isethionate salt

  • Excipients: Details not disclosed in public sources.

• Properties: Oral, selective CDK4/6 small-molecule inhibitor; halts cell-cycle progression at G₁-S checkpoint by reducing Rb phosphorylation, inhibiting tumor proliferation

• Packaging Specification:​ Tablets or capsules. Strengths unspecified in public sources; commonly administered as daily oral doses (e.g., 100 mg) in trials

• Storage:

  • As research compound: powder 3 years at −20 °C; stock solutions: −80 °C for 6 months or −20 °C for 1 month

  • Commercial tablet storage likely per label (typically room temperature)—not publicly specified.

• Expiry Date: ​Unknown

• Executive Standard: ​Unknown

• Approval Number: NMPA-approved for HR⁺/HER2⁻ metastatic breast cancer on December 31 2021; exact registration number not public

• Date of Revision: ​Unknown

• Manufacturer: Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Guidelines for the Use of Dalpiciclib Isethionate

• Dosage and Administration:

  • Oral, once daily; in Phase I/III combination with endocrine agents like fulvestrant or letrozole, common dose ~100 mg/day .

  • Taken with or without food; duration dependent on response and tolerance; regular monitoring recommended.

• Adverse Reactions:

  • Common: neutropenia, anemia, thrombocytopenia, fatigue, nausea, diarrhea, liver enzyme elevations

  • Less common: hepatotoxicity (requires liver monitoring), occasional QT prolongation, alopecia, rash

• Contraindications: Severe hepatic impairment, pregnancy, breastfeeding; known hypersensitivity; caution in patients with severe bone marrow suppression

• Precautions:

  • Monitor CBCs, liver function, cardiac symptoms (ECG); adjust dose or interrupt therapy for severe cytopenias or liver toxicity

Interactions

• Drug Interactions:​

• Metabolized via CYP3A4: avoid strong inhibitors (e.g., ketoconazole) or inducers (e.g., rifampin), which can alter drug exposure

• May have additive myelosuppressive or hepatotoxic effects with other chemotherapy or targeted agents.

Note:

• If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
• It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.