Lenalidomide

證據等級: L5 預測適應症: 6

目錄

  1. Lenalidomide
  2. Lenalidomide: From Undocumented Original Indication to Myeloid Leukemia
    1. One-Sentence Summary
    2. Quick Overview
    3. Why is This Prediction Reasonable?
    4. Clinical Trial Evidence
    5. Literature Evidence
    6. US Market Information
    7. Cytotoxicity
    8. Safety Considerations
    9. Conclusion and Next Steps
    10. Disclaimer

## 藥師評估報告

Lenalidomide: From Undocumented Original Indication to Myeloid Leukemia

One-Sentence Summary

Lenalidomide (DrugBank DB00480) is an oral immunomodulatory imide drug (IMiD); its original approved indication(s) are not recorded in this evidence pack. The TxGNN model predicts it may be effective for Myeloid Leukemia, with 50 clinical trials and 20 publications currently supporting this direction — though most of that trial base actually reflects lenalidomide’s established use in myelodysplastic syndrome (MDS) rather than de novo acute myeloid leukemia (AML).


Quick Overview

Item Content
Original Indication Not available in the evidence pack (no licenses/indication text on file)
Predicted New Indication Myeloid Leukemia
TxGNN Prediction Score 99.49%
Evidence Level L1 (≥2 completed Phase 3 RCTs identified — see caveat below)
US Market Status Not Marketed (未上市)
Number of NDAs 0
Recommended Decision Hold

Why is This Prediction Reasonable?

Currently, detailed mechanism of action data for lenalidomide is not available in this evidence pack. Based on publicly known pharmacology, lenalidomide is an immunomodulatory imide drug (IMiD) that binds cereblon (CRBN), promoting ubiquitination and degradation of the transcription factors IKZF1/IKZF3 — this is directly supported by literature in the evidence set (PMID 39881283: “The histone demethylase KDM5C enhances the sensitivity of acute myeloid leukemia cells to lenalidomide by stabilizing cereblon”). Through this mechanism it exerts antiproliferative, anti-angiogenic, and immune-stimulatory (NK/T-cell activating) effects.

Lenalidomide’s best-established hematologic use is in myelodysplastic syndrome (MDS), including MDS with deletion 5q — a disease on the same myeloid differentiation spectrum as AML, and one that frequently transforms into AML. The evidence pool for this predicted indication is dominated by MDS trials (including the two completed Phase 3 RCTs), with a substantial secondary layer of Phase 1/2 studies testing lenalidomide directly in AML, largely in combination with azacitidine, cytarabine-based chemotherapy, or as post-transplant/post-remission maintenance.

Mechanistically this extension is plausible: MDS and AML share overlapping myeloid clonal biology, and lenalidomide’s immunomodulatory and anti-angiogenic activity has already shown clinical signal in AML settings (post-transplant relapse, maintenance therapy, and combination regimens). However, the strongest (Phase 3) evidence in the pack is for MDS, not AML specifically — direct AML evidence remains Phase 1/2 in scale, which should temper confidence in reading this as an AML-specific L1 signal.


Clinical Trial Evidence

Trial Number Phase Status Enrollment Key Findings
NCT00179621 Phase 3 Completed 205 Lenalidomide (10mg/5mg) vs. placebo in RBC transfusion-dependent low/int-1 risk MDS with del(5q)
NCT01029262 Phase 3 Completed 239 Lenalidomide vs. placebo in transfusion-dependent anemia, low/int-1 risk MDS without del(5q)
NCT01358734 Phase 2 Completed 88 Lenalidomide vs. sequential azacitidine+lenalidomide vs. azacitidine alone in older newly-diagnosed AML
NCT01743859 Phase 2 Completed 37 Sequential azacitidine+lenalidomide in relapsed/refractory AML and high-risk MDS
NCT01772420 Phase 2 Completed 52 Lenalidomide + eltrombopag for symptomatic anemia in low/int-1 risk MDS
NCT02126553 Phase 2 Completed 29 Lenalidomide maintenance in high-risk AML patients in remission
NCT03118466 Phase 2 Completed 41 Lenalidomide + MEC (mitoxantrone/etoposide/cytarabine) in relapsed/refractory AML
NCT00352001 Phase 1/2 Completed 37 Lenalidomide + azacitidine in advanced MDS
NCT02472691 Phase 2 Completed 50 Lenalidomide + azacitidine + donor lymphocyte infusion for MDS/CMML/AML relapse post allo-SCT
NCT00360672 Phase 2 Completed 27 Lenalidomide in relapsed/refractory AML or high-risk MDS with chromosome 5 abnormalities

Literature Evidence

PMID Year Type Journal Key Findings
35277655 2022 RCT Leukemia Randomized Phase II study of azacitidine ± lenalidomide in higher-risk MDS/AML with del(5q)
30653424 2019 Trial J Clin Oncol Combination lenalidomide + azacitidine as salvage therapy after allo-SCT relapse in AML
37259567 2023 Trial Haematologica Azalena-Trial: azacitidine + lenalidomide + DLI for post-transplant relapse of MDS/AML/CMML
31009835 2019 Trial Leukemia Research Sequential azacitidine + lenalidomide in relapsed/refractory AML with predictive modeling
34955443 2022 Trial J Geriatric Oncology Phase Ib lenalidomide as post-remission therapy in older AML patients
40250191 2025 Trial Leukemia Research Phase I lenalidomide + bortezomib for AML/MDS relapsing after allo-SCT
34471239 2021 Trial Bone Marrow Transplant Safety and tolerability of lenalidomide maintenance post-transplant in AML/high-risk MDS
31221030 2019 Systematic Review/Meta-analysis Hematology (Amsterdam) Efficacy and adverse events of azacitidine+lenalidomide in AML, MDS, CMML
37874917 2023 Review Blood Clinical decision-making and treatment of myelodysplastic syndromes
24656536 2014 Review Lancet Myelodysplastic syndromes overview, including progression to AML

US Market Information

Not currently marketed — the evidence pack records zero licenses/NDAs and a market status of “Not Marketed” (未上市).


Cytotoxicity

Lenalidomide is an antineoplastic agent used in hematologic malignancies (MDS, and investigationally AML), so this section applies.

Item Content
Cytotoxicity Classification Targeted therapy — immunomodulatory imide drug (IMiD), not a conventional cytotoxic agent
Myelosuppression Risk Please refer to the package insert warnings and precautions
Emetogenicity Classification Please refer to the package insert warnings and precautions
Monitoring Items Please refer to the package insert warnings and precautions
Handling Protection Please refer to the package insert warnings and precautions

Safety Considerations

Please refer to the package insert for safety information.


Conclusion and Next Steps

Decision: Hold

Rationale:

  • A Blocking data gap (missing TFDA label warnings/contraindications) prevents entry into the S1 safety pre-assessment stage, and the drug currently has no market presence or license record in this jurisdiction. While the evidence base is large (50 trials, 20 publications, including 2 completed Phase 3 RCTs), that Phase 3 evidence is anchored in MDS rather than AML itself, so it does not by itself justify proceeding without a safety review.

To proceed, the following is needed:

  • TFDA label/package insert (warnings, contraindications) — download and parse from the TFDA website (DG001, Blocking)
  • Mechanism of action detail from DrugBank API to support mechanistic-relevance analysis (DG002, High)
  • A dedicated review of AML-specific (vs. MDS-specific) trial evidence to confirm whether Phase 3-level support genuinely extends to the “myeloid leukemia” indication or is primarily attributable to lenalidomide’s existing MDS approval

    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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