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.

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

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.