Datopotamab Deruxtecan Dosage

Medically reviewed by Drugs.com. Last updated on Feb 18, 2025.

Usual Adult Dose for Breast Cancer

6 mg/kg IV every 3 weeks (21-day cycle)
Maximum dose: 540 mg/dose
Duration of therapy: Until disease progression or unacceptable toxicity

Comments:

• First infusion: Administer over 90 minutes; observe patients during the infusion and for at least 1 hour after the initial dose for signs/symptoms of infusion-related reactions.
• Second infusion: If first infusion was tolerated, administer over 30 minutes; observe patients during the infusion and for at least 1 hour after infusion.
• Subsequent infusions: Administer over 30 minutes if prior infusions were tolerated; observe patients during the infusion and for at least 30 minutes after infusion.

Use: For the treatment of patients with unresectable or metastatic, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative (immunohistochemistry [IHC] 0, IHC 1+, or IHC 2+/in situ hybridization [ISH]-) breast cancer who have received prior endocrine-based therapy and chemotherapy for unresectable or metastatic disease

Renal Dose Adjustments

Mild to moderate renal dysfunction (CrCl 30 to less than 90 mL/min): No adjustment recommended
Severe renal dysfunction (CrCl less than 30 mL/min): Data not available

Comments:

• Patients with renal dysfunction should be monitored for increased adverse reactions (including respiratory reactions).

Liver Dose Adjustments

Mild liver dysfunction (total bilirubin up to 1 times the upper limit of normal [1 x ULN] and AST greater than ULN or total bilirubin greater than 1 to 1.5 x ULN and any AST): No adjustment recommended
Moderate liver dysfunction (total bilirubin greater than 1.5 to 3 x ULN and any AST): Limited data available; monitoring recommended
Severe liver dysfunction (total bilirubin greater than 3 x ULN and any AST): Data not available

Comments:

• Patients with moderate liver dysfunction should be monitored for increased adverse reactions.
• The recommended dosage has not been established for patients with severe liver dysfunction.

Dose Adjustments

DOSAGE MODIFICATIONS FOR ADVERSE REACTIONS:

• Do not re-escalate the dose of this drug after a dose reduction.
• Permanently discontinue this drug in patients unable to tolerate 3 mg/kg IV every 3 weeks.

Recommended Dose Reduction Levels:

• First dose reduction: 4 mg/kg IV every 3 weeks
• Maximum dose: 360 mg/dose
• Second dose reduction: 3 mg/kg IV every 3 weeks
• Maximum dose: 270 mg/dose
• Third dose reduction: Permanently discontinue.

Interstitial Lung Disease (ILD)/Pneumonitis:

• Asymptomatic ILD/pneumonitis (grade 1): Withhold this drug until ILD/pneumonitis is completely resolved, then:
• If resolved in 28 days or less: Maintain current dose.
• If resolved in more than 28 days: Reduce 1 dose level.
• Consider corticosteroids as soon as ILD/pneumonitis is suspected.
• Symptomatic ILD/pneumonitis (grade 2 or higher): Permanently discontinue.
• Administer corticosteroids as soon as ILD/pneumonitis is suspected.

Keratitis:

• Nonconfluent superficial keratitis: Monitor.
• Confluent superficial keratitis, a cornea epithelial defect, or 3-line or more loss in best corrected visual acuity: Withhold until improved or resolved, then maintain at the same dose level or consider dose reduction.
• Corneal ulcer, stromal opacity, or best corrected distance visual acuity 20/200 or worse: Withhold until improved or resolved, then reduce by 1 dose level.
• Corneal perforation: Permanently discontinue.

Stomatitis:

• Grade 1: Optimize prophylactic and supportive medications.
• Grade 2: Withhold until resolved to lower than grade 1.
• First occurrence: Restart at the same dose level.
• If recurrent: Consider restarting at reduced dose level.
• Grade 3: Withhold until resolved to grade 1 or lower.
• Restart at reduced dose level.
• Grade 4: Permanently discontinue.

Infusion-Related Reactions:

• Grade 1: Reduce the infusion rate of this drug by 50% if infusion-related reaction is suspected and monitor patient closely.
• Grade 2: Interrupt infusion of this drug and administer supportive care medications.
• If the event resolves or improves to grade 1: Restart the infusion at 50% rate.
• Administer all subsequent infusions at the reduced rate.
• Grade 3 or 4: Permanently discontinue this drug.

Other Nonhematologic Adverse Reactions:

• Grade 3: Withhold dose until resolved to grade 1 or lower or baseline.
• Restart at reduced dose level.
• Grade 4: Permanently discontinue this drug.

Precautions

CONTRAINDICATIONS: None

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:

• Administer this drug in a setting where cardiopulmonary resuscitation medication and equipment are available.
• Administer as an IV infusion only; do NOT administer as an IV push or bolus.
• Administer with an infusion line and tubing set made of polyvinyl chloride, polybutadiene, or low-density polyethylene.
• Administer with a 0.2-micron in-line polytetrafluoroethylene, polyethersulfone, or nylon 66 filter.
• Cover the infusion bag to protect from light during administration.
• The maximum time from reconstitution of the vial through the end of administration should not exceed 24 hours; discard if storage time exceeds these limits.
• Do not mix with other drugs or administer other drugs through the same IV line.
• Instruct the patient to hold ice chips or ice water in the mouth throughout the infusion of this drug.
• If a planned dose is missed or delayed, administer as soon as possible; do not wait until the next planned cycle. Adjust the administration schedule to maintain a 3-week interval between doses.

Premedication and Concomitant Medications:

• Administer this drug with the following premedication (with or without systemic corticosteroids) and concomitant medications.
• Eye drops (e.g., preservative-free lubricant eye drops): Administer at least 4 times a day and as needed.
• Mouthwash (e.g., steroid-containing mouthwash [dexamethasone oral solution 0.1 mg/mL] or equivalent): Administer 4 times a day and as needed.
• Antihistamine (e.g., IV or oral diphenhydramine [25 to 50 mg] or equivalent): Administer 30 to 60 minutes before each infusion.
• Antipyretic (e.g., IV or oral acetaminophen [650 to 1000 mg] or equivalent): Administer 30 to 60 minutes before each infusion.
• Antiemetics (e.g., IV or oral 5-HT3 serotonin receptor antagonist or appropriate alternatives): Administer before each infusion and thereafter as needed.

Storage requirements:

• Vials: Store in a refrigerator at 2C to 8C (36F to 46F) in the original carton to protect from light until time of reconstitution; do not freeze.
• Reconstituted solution: If not used immediately, refrigerate the solution in the original vial at 2C to 8C (36F to 46F) for up to 24 hours from time of reconstitution; protect vial from light; do not freeze or shake.
• Discard unused solution after 24 hours refrigerated.
• Diluted solution: Protect from light. If not used immediately, store at room temperature at up to 25C (77F) for up to 4 hours including preparation or in a refrigerator at 2C to 8C (36F to 46F) for up to 24 hours; do not freeze or shake.
• If prepared infusion solution was stored refrigerated: Allow to reach room temperature before administration, protected from light.

Reconstitution/preparation techniques:

• Reconstitute and further dilute this drug before IV infusion.
• The manufacturer product information should be consulted.

IV compatibility:

• Compatible: Sterile Water for Injection, 5% Dextrose Injection
• Compatible with infusion bag made of polyvinyl chloride or polyolefin (polypropylene or copolymer of ethylene and propylene)
• DO NOT use Sodium Chloride Injection.

General:

• This is a hazardous drug; follow applicable special handling and disposal procedures.

Monitoring:

• Gastrointestinal: For signs/symptoms of stomatitis
• General: For increased adverse reactions in patients with renal dysfunction or moderate liver dysfunction
• Ocular: Ophthalmic examination including visual acuity testing, slit lamp examination with fluorescein staining, intraocular pressure, and fundoscopy (at initiation of drug, annually during therapy, at end of therapy, and as clinically indicated); for ocular adverse reactions (during therapy)
• Respiratory: For new/worsening respiratory symptoms indicative of ILD/pneumonitis (during therapy)

Patient advice:

• Read the US FDA-approved patient labeling (Medication Guide).
• Contact your health care provider immediately for any of the following: cough, shortness of breath, fever, or other new/worsening respiratory symptoms.
• Contact your health care provider if you have any eye symptoms; use preservative-free lubricating eye drops several times a day and avoid use of contact lenses during therapy.
• Contact your health care provider if you have any symptoms of stomatitis. Use a steroid-containing mouthwash for prophylaxis and treatment of stomatitis; hold ice chips or ice water in your mouth throughout the infusion of this drug.
• Patients of childbearing potential: Inform your health care provider of a known/suspected pregnancy; use effective contraception during therapy and for 7 months after the last dose.
• Male patients with partners of childbearing potential: Use effective contraception during therapy and for 4 months after the last dose.
• Do not breastfeed during therapy and for 1 month after the last dose.

See also:

Further information

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