datopotamab deruxtecan

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Mild or moderate renal impairment (CCr 30–<90 mL/min) (↑ risk of interstitial lung disease (ILD)/pneumonitis);
Moderate hepatic impairment (total bilirubin >1.5–3 times upper limit of normal and any AST);
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: alopecia, rash, dry skin, hyperpigmentation, pruritus

EENT: dry eye, keratitis, ↑lacrimation, blepharitis, blurred vision, conjunctivitis, meibomian gland dysfunction, photophobia, visual impairment

F and E: hypocalcemia

GI: ↓appetite, ↑liver enzymes, abdominal pain, constipation, diarrhea, nausea, stomatitis, vomiting, dry mouth

GU: ↓fertility

Hemat: anemia, leukopenia, lymphopenia, neutropenia

Neuro: cough, fatigue, headache

Resp: ILD/PNEUMONITIS

Misc: infusion-related reactions

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

Lyophilized powder for injection: 100 mg/vial

Route/Dosage ⬆ ⬇

IV (Adults ≥90 kg): 540 mg every 3 wk; continue until disease progression or unacceptable toxicity.
IV (Adults <90 kg): 6 mg/kg every 3 wk; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Datopotamab deruxtecan is an antibody-drug conjugate consisting of datopotamab, a monoclonal antibody directed against Trop-2 (expressed on cancer cells), and DXd, a topoisomerase I inhibitor. After binding to Trop-2, datopotamab deruxtecan is internalized and releases DXd, which then leads to DNA damage and apoptosis.

Therapeutic effects:

Improved progression-free survival.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: monoclonal antibodies, enzyme inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Minimally distributed to extravascular tissues.

Metabolism/Excretion: Datapotamab is degraded into small peptides and amino acids via catabolic pathways; DXd is primarily metabolized by the CYP3A4 isoenzyme. Excretion pathway not characterized.

Half-Life: Datapotamab deruxtecan: 4.8 days; DXd: 5.5 days.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	rapid	end of infusion	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of datopotamab deruxtecan. Do not stop receiving drug without consulting health care provider. If an appointment is missed, contact health care provider as soon as possible to reschedule. Advise patient to read Medication Guide before starting and periodically during therapy in case of changes.
Explain need for continued medical follow-up to assess effectiveness and possible side effects of medication. Periodic eye exams will be needed.
May cause temporary blurred vision. Warn patient to avoid driving or other activities requiring clear vision until response to medication is known or until blurred vision resolves. Avoid use of contact lenses unless directed by eye care provider.
Instruct patient to notify health care provider or call 911 immediately to seek medical care if swelling of face, eyes, lips, or tongue or if difficulty swallowing or breathing occur.
Advise patient to report symptoms of ILD/pneumonitis (cough, shortness of breath, fever, other new or worsening respiratory symptoms).
Instruct patient to inspect oral mucosa for erythema and ulceration. If ulceration occurs, advise patient to use sponge brush and to rinse mouth with water after eating and drinking. Topical therapy may be used if mouth pain interferes with eating. Stomatitis pain may require treatment with opioid analgesics.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected and not to breastfeed during treatment and for 1 mo after last dose. Advise women of reproductive potential to use effective contraception during treatment and for 7 mo after last dose. Advise men with female partners of reproductive potential to use effective contraception during treatment and for 4 mo after last dose.

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Indications ⬇

Contraind./Precautions ⬆ ⬇