Mechlorethamine

證據等級: L5 預測適應症: 3

目錄

  1. Mechlorethamine
  2. Mechlorethamine: From Hodgkin Lymphoma to Lymph Node Cancer
    1. One-Sentence Summary
    2. Quick Overview
    3. Why is This Prediction Reasonable?
    4. Clinical Trial Evidence
    5. Literature Evidence
    6. Cytotoxicity
    7. Safety Considerations
    8. Conclusion and Next Steps
    9. Disclaimer

## 藥師評估報告

Mechlorethamine: From Hodgkin Lymphoma to Lymph Node Cancer

One-Sentence Summary

Mechlorethamine (nitrogen mustard) is a classic alkylating chemotherapy agent historically used as the backbone of the MOPP regimen for Hodgkin lymphoma and as a topical gel for cutaneous T-cell lymphoma (mycosis fungoides). The TxGNN model further predicts strong relevance to Lymph Node Cancer (score 99.43%), a use area that substantially overlaps with the drug’s established history rather than representing a wholly novel mechanism — supported by 50 matched clinical trial records and 20 publications, though most trials are indirect (lymphoma regimens using other agents) while the literature includes several historical RCTs of mechlorethamine-containing regimens.

Quick Overview

Item Content
Original Indication Hodgkin lymphoma (as part of the MOPP regimen); historical topical use in cutaneous T-cell lymphoma/mycosis fungoides — no structured Taiwan/US license data available to confirm current labeling
Predicted New Indication Lymph Node Cancer
TxGNN Prediction Score 99.43%
Evidence Level L2 (historical RCTs of mechlorethamine-based regimens exist for Hodgkin lymphoma; most matched ClinicalTrials.gov records are indirect)
US Market Status Not marketed (no active licenses on record)
Number of NDAs 0
Recommended Decision Hold

Why is This Prediction Reasonable?

Currently, detailed structured mechanism-of-action data is not available in this evidence pack. Based on known pharmacology, mechlorethamine is a bifunctional alkylating agent (the prototypical nitrogen mustard) that cross-links DNA strands and halts replication in rapidly dividing cells. It formed the backbone of the historic MOPP regimen (mechlorethamine, vincristine, procarbazine, prednisone), one of the first combination chemotherapy protocols to achieve durable remission in Hodgkin lymphoma, and a topical 0.016% gel formulation (chlormethine/mechlorethamine) is used for cutaneous T-cell lymphoma/mycosis fungoides — both malignancies of the lymphatic system.

Lymph node cancer (lymphoma broadly) is therefore mechanistically and clinically close to mechlorethamine’s already-established use. The TxGNN prediction largely reinforces a decades-old, clinically validated application rather than identifying a genuinely new pharmacological pathway. This explains why the literature evidence (MOPP-regimen randomized trials) is comparatively strong, even though most matched ClinicalTrials.gov records in this pack involve adjacent but different regimens (rituximab, bendamustine, CAR-T, venetoclax, etc.) rather than mechlorethamine itself.

Clinical Trial Evidence

Note: none of the matched ClinicalTrials.gov records use mechlorethamine directly — they reflect the broader lymphoma/lymph-node-cancer treatment landscape retrieved by the search, not direct trials of this drug.

Trial Number Phase Status Enrollment Key Findings
NCT02005471 Phase 3 Completed 389 Venetoclax + rituximab vs. bendamustine + rituximab in relapsed/refractory CLL — not a mechlorethamine trial
NCT02162771 Phase 3 Completed 140 Biosimilar rituximab (CT-P10) vs. Rituxan with CVP in advanced follicular lymphoma
NCT01889069 Phase 3 Completed 159 Subcutaneous rituximab in untreated CD20+ DLBCL/follicular lymphoma
NCT06191744 Phase 3 Recruiting 1095 Epcoritamab + lenalidomide/rituximab vs. chemoimmunotherapy in untreated follicular lymphoma
NCT00562965 Phase 3 Terminated 29 Inotuzumab ozogamicin + rituximab vs. investigator’s choice in relapsed/refractory follicular NHL
NCT01008462 Phase 2 Completed 16 Sequential autologous/haploidentical allogeneic HCT for high-risk lymphoma, myeloma, or CLL
NCT00924326 Phase 1/2 Completed 43 Anti-CD19 CAR T-cell therapy in B-cell lymphoma
NCT00974233 Phase 2 Completed 34 Bendamustine + rituximab induction with lenalidomide/rituximab maintenance in relapsed/refractory CLL/SLL
NCT00450801 Phase 2 Completed 22 Rituximab + MACLO/IVAM chemotherapy in previously untreated mantle cell lymphoma
NCT00911183 Phase 2 Completed 67 Rituximab-CHOP-type regimen in frail elderly diffuse large B-cell lymphoma

Literature Evidence

PMID Year Type Journal Key Findings
3352775 1988 RCT NCI Monographs EORTC H5 trial: mantle irradiation + mechlorethamine/vincristine/procarbazine/prednisone (MVPP) vs. total nodal irradiation in stage I–II Hodgkin’s disease
7509381 1994 RCT J Clin Oncol Randomized comparison of MOPP alone vs. MOPP/ABVD alternation in stage IIIB/IV Hodgkin’s disease
2436740 1987 Cohort Cancer MOPP chemotherapy with/without involved-field radiotherapy in 37 children with Hodgkin’s disease
7540419 1995 Cohort Annals of Oncology Hybrid MOPP/ABVD plus radiotherapy in advanced Hodgkin’s disease
35393251 2022 Retrospective Clin Lymphoma Myeloma Leuk Chlormethine/mechlorethamine 0.016% gel as maintenance therapy in mycosis fungoides
6809030 1982 Retrospective Br J Dermatol Topical mechlorethamine (HN2) among treatments in 92 cutaneous T-cell lymphoma patients
24438970 2014 Review J Am Acad Dermatol Prognosis and management (part II) of mycosis fungoides/Sézary syndrome
10473086 1999 Mechanistic Clin Cancer Res O6-alkylguanine-DNA alkyltransferase and resistance to alkylating agents (incl. mechlorethamine) in cutaneous T-cell lymphoma
31894937 2020 Review American Family Physician General overview of lymphoma diagnosis and treatment
20564093 2010 Cohort Cancer Characteristics and outcomes of Hodgkin lymphoma involving nodal and extranodal head/neck sites

Cytotoxicity

Item Content
Cytotoxicity Classification Conventional cytotoxic (alkylating agent, nitrogen mustard class)
Myelosuppression Risk High — nitrogen mustards are well-documented potent bone-marrow suppressants at the class level; product-specific hematologic toxicity data is not available in this evidence pack (refer to package insert)
Emetogenicity Classification High (for IV formulation; class-level classification per standard oncology emetogenicity scales)
Monitoring Items CBC with differential and platelets, liver and renal function, injection/application site monitoring (vesicant potential)
Handling Protection Cytotoxic/vesicant drug handling precautions expected (closed-system transfer devices, PPE, spill kit); specific TFDA/DrugBank handling requirements not confirmed in this evidence pack

Safety Considerations

Please refer to the package insert for safety information.

Conclusion and Next Steps

Decision: Hold

Rationale: A Blocking-severity data gap (TFDA/regulatory label warnings and contraindications) prevents safety pre-screening (S1), and the drug currently has no active market licenses on record. In addition, the repurposing signal for lymph node cancer largely reconfirms mechlorethamine’s already-established historical role (MOPP regimen, topical CTCL use) rather than identifying a genuinely novel mechanism, so this candidate does not require de novo efficacy proof but does require safety documentation before advancing.

To proceed, the following is needed:

  • TFDA/regulatory package insert (warnings, contraindications) — Blocking gap
  • Structured mechanism-of-action data from DrugBank — High-priority gap
  • Confirmation of current formulation availability (IV vs. topical gel) and market access pathway
  • Drug-drug interaction profile validation

    Disclaimer

This content is for research purposes only and does not constitute medical advice. Clinical validation is required before any clinical application.



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