Datopotamab Deruxtecan

Datopotamab deruxtecan-dlnk, is a Trop-2-directed antibody-drug conjugate. The antibody is a humanized anti-Trop2 IgG1.

• DATROWAY is a Trop-2-directed antibody and topoisomerase inhibitor conjugate indicated for the treatment of: adult patients with locally advanced or metastatic epidermal growth factor receptor (EGFR)-mutated non-small cell lung cancer (NSCLC) who have received prior EGFR-directed therapy and platinum-based chemotherapy. ( 1.1 ) This indication is approved under accelerated approval based on objective response rate and duration of response [see Clinical Studies (14.1) ] .ICD-10: C34.90

• None. None.contraindicated

Reconstitute DATROWAY with Sterile Water for Injection. ( 2.5 ) Dilute with 5% Dextrose Injection. ( 2.5 ) For intravenous infusion only. Do not administer as an intravenous push or bolus. DO NOT use Sodium Chloride Injection, USP. ( 2.5 ) Premedicate to reduce the risk of infusion reactions and nausea and vomiting. ( 2.3 ) The recommended dosage of DATROWAY is 6 mg/kg (up to a maximum of 540 mg for patients ≥90 kg) given as an intravenous infusion once every 3 weeks (21-day cycle) until disease progression or unacceptable toxicity. ( 2.3 , 2.4 ) 2.1 Patient Selection Select patients with locally advanced or metastatic NSCLC for treatment with DATROWAY based on the presence of epidermal growth factor receptor (EGFR) mutations in tumor or plasma specimens [see Clinical Studies (14.1) ] . Testing may be performed at any time from initial diagnosis and does not need to be repeated once EGFR mutation status has been established. 2.2 Recommended Dosage The recommended dosage of DATROWAY is 6 mg/kg (up to a maximum of 540 mg for patients ≥90 kg) administered as an intravenous infusion once every 3 weeks (21-day cycle) until disease progression or unacceptable toxicity. If a planned dose is delayed or missed, administer as soon as possible; do not wait until the next planned cycle. Adjust the schedule of administration to maintain a 3-week interval between doses.

Interstitial Lung Disease (ILD) and Pneumonitis: DATROWAY can cause severe and fatal cases of ILD/pneumonitis. Monitor for new or worsening signs and symptoms of ILD/pneumonitis. If ILD/pneumonitis is suspected, withhold DATROWAY and initiate corticosteroids. Permanently discontinue DATROWAY in patients with confirmed Grade 2 or higher ILD/pneumonitis. ( 5.1 ) Ocular Adverse Reactions: DATROWAY can cause ocular adverse reactions including dry eye, keratitis, blepharitis, meibomian gland dysfunction, increased lacrimation, conjunctivitis, and blurred vision. Monitor patients for ocular adverse reactions during treatment with DATROWAY. Advise patients to use preservative-free lubricating eye drops and to avoid using contact lenses during treatment with DATROWAY. Withhold, reduce the dose, or permanently discontinue DATROWAY based on the severity of ocular adverse reactions. Refer patients to an eye care professional for any new or worsening ocular signs and symptoms. ( 2.3 , 2.4 , 5.2 ) Stomatitis/Oral Mucositis: DATROWAY can cause stomatitis, including mouth ulcers and oral mucositis. Advise patients to use a steroid-containing mouthwash when starting treatment and to hold ice chips or ice water in mouth during the infusion of DATROWAY. Withhold, reduce the dose, or permanently discontinue DATROWAY based on severity. ( 2.3 , 2.4 , 5.3 ) Embryo-Fetal Toxicity : DATROWAY can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception.

The following clinically significant adverse reactions are described elsewhere in the labeling: Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.1) ] Ocular Adverse Reactions [see Warnings and Precautions (5.2) ] Stomatitis [see Warnings and Precautions (5.3) ] The most common adverse reactions (≥20%), including laboratory abnormalities, in patients with: EGFR-mutated NSCLC were stomatitis, nausea, alopecia, fatigue, decreased hemoglobin, decreased lymphocytes, constipation, increased calcium, increased AST, decreased white blood cell count, increased lactate dehydrogenase, musculoskeletal pain, decreased appetite, increased ALT, and rash. ( 6.1 ) TNBC were stomatitis, increased amylase, nausea, alopecia, decreased hemoglobin, decreased white blood cells, constipation, decreased calcium, decreased lymphocytes, fatigue, decreased neutrophils, increased ALT, increased AST, dry eye, keratitis, decreased albumin, vomiting, musculoskeletal pain, decreased sodium, and increased blood alkaline phosphatase. ( 6.1 ) HR-positive, HER2-negative breast cancer were stomatitis, nausea, fatigue, decreased leukocytes, decreased calcium, alopecia, decreased lymphocytes, decreased hemoglobin, constipation, decreased neutrophils, dry eye, vomiting, increased ALT, keratitis, increased AST, and increased alkaline phosphatase. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Daiichi Sankyo, Inc. at 1-877-437-7763 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Lactation: Advise not to breastfeed. ( 8.2 ) Infertility: May impair fertility in males and females. ( 8.3 ) 8.1 Pregnancy Risk Summary Based on its mechanism of action, DATROWAY can cause embryo-fetal harm when administered to a pregnant woman because the topoisomerase inhibitor component of DATROWAY, DXd, is genotoxic and affects actively dividing cells [see Clinical Pharmacology (12.1) , Nonclinical Toxicology (13.1) ] . There are no available data on the use of DATROWAY in pregnant women to inform a drug-associated risk. Advise patients of the potential risks to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data There were no animal reproductive or developmental toxicity studies conducted with datopotamab deruxtecan-dlnk. 8.2 Lactation Risk Summary There are no data regarding the presence of datopotamab deruxtecan-dlnk or its metabolites in human milk, the effects on the breastfed child, or the effects on milk production. Because of the potential for serious adverse reactions in a breastfed child, advise women not to breastfeed during treatment with DATROWAY and for 1 month after the last dose.

Metabolism

Datopotamab deruxtecan-dlnk and DXd exposure after the first dose of the approved recommended dosage of cycle 1 are provided in Table 10. Datopotamab deruxtecan-dlnk and released DXd maximum concentration (C max ) and area under the time-concentration curve (AUC) increases proportionally over a dose range of 4 mg/kg to 10 mg/kg (approximately 0.7 to 1.7 times the approved recommended dosage).

• Jan 17, 2025BLABLA761394Daiichi Sankyo Inc

1. 1Disease Progression8820%
2. 2Stomatitis7116%
3. 3Off Label Use7016%
4. 4No Adverse Event429.4%
5. 5Death255.6%
6. 6Nausea235.1%
7. 7Fatigue184.0%
8. 8Interstitial Lung Disease163.6%
9. 9Dry Eye143.1%
10. 10Infusion Related Reaction143.1%
11. 11Dyspnoea132.9%
12. 12Weight Decreased132.9%
13. 13Alopecia112.5%
14. 14Rash112.5%
15. 15Cough102.2%

The 10 most recently updated of 45 ClinicalTrials.gov registrations naming Datopotamab Deruxtecan as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Study of Dato-DXd Plus Pembrolizumab vs Pembrolizumab Alone in the First-line Treatment of Subjects With Advanced or Metastatic NSCLC Without Actionable Genomic Alterations
  Active not recruiting · Phase 3 · Interventional · 740 enrolled · Daiichi Sankyo
  NCT05215340updated 2026-06-12
• A Study of AZD3470, a PRMT5 Inhibitor, Given as Monotherapy and in Combination in Patients With MTAP Deficient Advanced/Metastatic Solid Tumors
  Recruiting · Phase 1 · Phase 2 · Interventional · 334 enrolled · AstraZeneca
  NCT06130553updated 2026-06-11
• Study of Datopotamab Deruxtecan Plus Carboplatin or Cisplatin Versus Gemcitabine Plus Carboplatin or Cisplatin in Participants With Locally Advanced or Metastatic Urothelial Carcinoma
  Recruiting · Phase 2 · Phase 3 · Interventional · 630 enrolled · Daiichi Sankyo
  NCT07129993updated 2026-06-08
• Study of AZD9574 as Monotherapy and in Combination With Anti-cancer Agents in Participants With Advanced Solid Malignancies
  Recruiting · Phase 1 · Phase 2 · Interventional · 695 enrolled · AstraZeneca
  NCT05417594updated 2026-06-02
• Phase III Study of Datopotamab Deruxtecan Versus Docetaxel in Previously Treated TROP2-positive Advanced or Metastatic Non-squamous NSCLC Without Actionable Genomic Alterations
  Recruiting · Phase 3 · Interventional · 400 enrolled · AstraZeneca
  NCT07291037updated 2026-06-01
• Neoadjuvant and Adjuvant Treatment in Resectable Non-small Cell Lung Cancer
  Recruiting · Phase 2 · Interventional · 630 enrolled · AstraZeneca
  NCT05061550updated 2026-05-22
• Investigating Datopotamab Deruxtecan Plus Durvalumab Versus Datopotamab Deruxtecan in Patients With PDL1-negative Metastatic Triple-negative Breast Cancer
  Recruiting · Phase 2 · Interventional · 140 enrolled · Queen Mary University of London
  NCT06954480updated 2026-05-22
• A Phase III, Randomised Study of Adjuvant Dato-DXd in Combination With Rilvegostomig or Rilvegostomig Monotherapy Versus Standard of Care, Following Complete Tumour Resection, in Participants With Stage I Adenocarcinoma NSCLC Who Are ctDNA-positive or Have High-risk Pathological Features
  Active not recruiting · Phase 3 · Interventional · 25 enrolled · AstraZeneca
  NCT06564844updated 2026-05-22
• Phase III, Open-label, Study of First-line Dato-DXd in Combination With Rilvegostomig for Advanced Non-squamous NSCLC With High PD-L1 Expression (TC ≥ 50%) and Without Actionable Genomic Alterations
  Recruiting · Phase 3 · Interventional · 675 enrolled · AstraZeneca
  NCT06357533updated 2026-05-18
• A Study of Dato-DXd Versus Investigator's Choice Chemotherapy in Patients With Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer, Who Are Not Candidates for PD-1/PD-L1 Inhibitor Therapy (TROPION-Breast02)
  Active not recruiting · Phase 3 · Interventional · 644 enrolled · AstraZeneca
  NCT05374512updated 2026-05-15

Frequently asked questions

How does Datopotamab Deruxtecan work?

Datopotamab deruxtecan-dlnk, is a Trop-2-directed antibody-drug conjugate. The antibody is a humanized anti-Trop2 IgG1.

What is Datopotamab Deruxtecan used for?

According to FDA labeling, Datopotamab Deruxtecan carries indications including: DATROWAY is a Trop-2-directed antibody and topoisomerase inhibitor conjugate indicated for the treatment of: adult patients with locally advanced or metastatic epidermal growth factor receptor (EGFR)-mutated non-small cell lung cancer (NSCLC) who have received prior EGFR-directed therapy and platinum-based chemotherapy. ( 1.1 ) This indication is approved under accelerated approval based on objective response rate and duration of response [see Clinical Studies (14.1) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Datopotamab Deruxtecan?

Datopotamab Deruxtecan is classified as Other monoclonal antibodies and antibody drug conjugates, Antibody Interactions, Topoisomerase Inhibitors, Decreased DNA Integrity, Increased Cellular Death.

What are the brand names for Datopotamab Deruxtecan?

Datopotamab Deruxtecan is marketed under brand names including Datroway.

What are the contraindications for Datopotamab Deruxtecan?

Datopotamab Deruxtecan labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.