15 ADC Drugs: Usage and Dosage Summary

15 ADC Drugs: Usage and Dosage Summary
Currently, 15 ADC drugs have been approved globally, of which 6 are approved in China, namely Enfortumab vedotin, Brentuximab vedotin, Trastuzumab deruxtecan, Gemtuzumab ozogamicin, Sacituzumab govitecan, and Loncastuximab tesirine.
This article provides a brief summary of the currently approved ADC drugs, the types of tumors they are suitable for, and how to use them.
1. Enfortumab vedotin (Target: HER-2)
Indications
Adjuvant treatment of breast cancer: Monotherapy is suitable for HER2-positive early breast cancer patients who have residual invasive lesions after receiving taxane-based neoadjuvant therapy combined with trastuzumab.
Treatment of metastatic breast cancer: Monotherapy is suitable for HER2-positive, locally advanced or metastatic breast cancer patients who are not amenable to surgery and have received treatment with taxanes and trastuzumab. Patients should have one of the following conditions: previously treated for locally advanced or metastatic breast cancer or experienced disease recurrence within 6 months after adjuvant therapy or completion of adjuvant therapy.
Rational Drug Use
The recommended dosage is 3.6 mg/kg, once every 3 weeks (21 days per cycle), administered intravenously.
Enfortumab vedotin (T-DM1) and trastuzumab are different drugs and should not be substituted in clinical applications.
Dilute in 250 ml of 0.45% or 0.9% sodium chloride; 5% glucose solution should not be used for dilution, as it can cause protein aggregation, and it should not be mixed or diluted with other drugs. If using 0.9% sodium chloride for infusion, a 0.2/0.22μm in-line polyethersulfone filter is required. Once prepared for infusion, it should be administered immediately. If not used immediately, the infusion can be stored in a refrigerator at 2-8°C for up to 24 hours. Do not freeze or shake the infusion bag during storage.
2. Brentuximab vedotin (Target: CD30)
Indications
For patients with relapsed or refractory systemic anaplastic large cell lymphoma. For patients with relapsed or refractory classic Hodgkin lymphoma. For patients with primary cutaneous anaplastic large cell lymphoma or mycosis fungoides who have previously received systemic treatment.
Rational Drug Use
The recommended dosage is 1.8 mg/kg, administered intravenously for more than 30 minutes, once every 3 weeks. It should not be given as an intravenous push or rapid infusion. It can only be administered through a dedicated intravenous line and should not be mixed with other drugs.
Extract an appropriate volume of reconstituted brentuximab vedotin into an infusion bag containing 9 mg/mL (0.9%) sodium chloride solution, achieving a final concentration of brentuximab vedotin of 0.4-1.2 mg/mL. The recommended dilution volume is 150 mL. 5% dextrose injection or lactated Ringer’s solution may also be used for diluting reconstituted brentuximab vedotin.
Avoid use in patients with severe renal impairment (creatinine clearance <30 ml/min).
3. Trastuzumab deruxtecan (Target: HER-2)
Indications
For patients with HER2-overexpressing locally advanced or metastatic gastric cancer (including gastroesophageal junction adenocarcinoma) who have received at least 2 lines of systemic chemotherapy. HER2 overexpression is defined as a HER2 immunohistochemistry result of 2+ or 3+, regardless of FiSH/CiSH amplification.
Rational Drug Use
The recommended dosage is 2.5 mg/kg, administered intravenously every 2 weeks, lasting 30-90 minutes (usually recommended around 60 minutes).
No dose adjustment is required for patients with mild hepatic impairment; the effects of moderate to severe hepatic impairment on the pharmacokinetics of this drug have not yet been studied; no dose adjustment is required for patients with mild to moderate renal impairment, and there is no research data on patients with severe renal impairment.
4. Gemtuzumab ozogamicin (Target: CD33)
Indications
For acute myeloid leukemia (AML).
Rational Drug Use
The recommended dosage is 3 mg/m2, for intravenous infusion only, not for rapid intravenous injection, preferably completed via a large vein over 2 hours.
5. Moxetumomab pasudotox (Target: CD22)
Indications
For the treatment of adult patients with relapsed or refractory hairy cell leukemia (HCL).
Rational Drug Use
The recommended dosage is 0.04 mg/kg, administered intravenously for more than 30 minutes, on days 1, 3, and 5 of a 28-day cycle, until six cycles of treatment or disease progression or unacceptable toxicity. Not recommended for patients with severe renal impairment.
6. Polatuzumab vedotin (Target: CD79b)
Indications
For the treatment of adult patients with relapsed or refractory (R/R) diffuse large B-cell lymphoma (DLBCL) who have received at least two lines of therapy.
Rational Drug Use
The recommended dosage is 1.8 mg/kg, administered intravenously every 21 days, in combination with bendamustine and rituximab for 6 cycles. Antihistamines and antipyretics should be taken at least 30 minutes before Polatuzumab vedotin administration.
7. Enfortumab vedotin (Target: Nectin-4)
Indications
For adult patients with locally advanced or metastatic urothelial carcinoma who have previously received PD-1 or PD-L1 inhibitors, and in the context of neoadjuvant/adjuvant, locally advanced, or metastatic platinum-containing chemotherapy.
Rational Drug Use
The recommended dosage is 1.25 mg/kg (maximum dose of 125 mg), administered intravenously on days 1, 8, and 15 of a 28-day cycle over 30 minutes, until disease progression or unacceptable toxicity.
Avoid use in patients with moderate or severe liver dysfunction.
8. Belantamab mafodotin (Target: B-cell maturation antigen)
Indications
For the treatment of adult patients with relapsed or refractory multiple myeloma who have previously received at least 4 lines of therapy (including anti-CD38 monoclonal antibodies, proteasome inhibitors, and immunomodulators).
Rational Drug Use
The recommended dosage is 2.5 mg/kg, administered intravenously every 3 weeks for about 30 minutes, until disease progression or unacceptable toxicity; the recommended dosage based on adverse reactions is 1.9 mg/kg intravenously every 3 weeks; stop if unable to tolerate 1.9 mg/kg dosage.
9. Cetuximab saratolacan (Target: EGFR)
Indications
For the treatment of unresectable locally advanced or recurrent head and neck cancer.
10. Loncastuximab tesirine (Target: CD19)
Indications
For the treatment of adult patients with relapsed or refractory (R/R) large B-cell lymphoma (LBCL) who have received at least 2 lines of systemic therapy, including diffuse large B-cell lymphoma (DLBCL), and high-grade B-cell lymphoma originating from low-grade lymphoma.
11. Tisotumab vedotin-tftv
Indications
For the treatment of adult patients with recurrent or metastatic cervical cancer who have progressed during or after chemotherapy.
Rational Drug Use
The recommended dosage is 2 mg/kg (up to 200 mg for patients ≥100 kg) administered intravenously every 3 weeks, infused over 30 minutes, until disease progression or unacceptable toxicity.
12. Mirvetuximab soravtansine (Target: Folate receptor alpha)
Indications
For the treatment of adult patients with folate receptor alpha (FRα) positive platinum-resistant epithelial ovarian cancer, fallopian tube cancer, or primary peritoneal cancer who have previously received 1-3 lines of systemic therapy.

Conclusion

Currently, there are 15 ADC drugs approved globally, with 5 approved in China. It is believed that with the continuous development and progress of drugs, more ADC drugs will be approved in China, bringing hope for treatment to more cancer patients.

Author: Jin Haobing;Editor: Cai Yuhan

Cover Image: Zcool Hailuo PLUS

Submission: [email protected]

15 ADC Drugs: Usage and Dosage Summary

References

1. Fu Z, Li S, Han S, et al. Antibody drug conjugate: the “biological missile” for targeted cancer therapy. [J]. Signal Transduct Target Ther, 2022.

2. Expert consensus on the clinical application of antibody-drug conjugates for malignant tumors (2020 edition)

3. Drug instructions

4. Guidelines for the clinical application of novel anti-tumor drugs (2022 edition)

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