Molecular Oncology · Hematological Malignancies

Emerging Research in Chronic Lymphocytic Leukemia

2024–2025 Clinical & Translational Update — BTK Degraders, Fixed-Duration Combinations, Bispecific Antibodies, CAR-T & MRD-Guided Strategies

4.6 per 100k / yr incidence
215k living with CLL — US 2024
70 yrs median age at dx
1.9:1 male : female ratio

CLL remains the most common leukemia in adults in the Western world. The treatment landscape has been fundamentally transformed over the past decade — from chemoimmunotherapy to oral targeted agents — and is now entering a new era defined by fixed-duration combinations, next-generation kinase degraders, and immunotherapeutic strategies. The central challenge in 2025 is managing patients who become double-refractory to both BTK and BCL-2 inhibitors.

1

Current & Emerging Therapeutic Classes


Approved

BTK Inhibitors (BTKi)

Ibrutinib · Acalabrutinib · Zanubrutinib · Pirtobrutinib (non-covalent)

  • Block BCR signalling via irreversible covalent BTK binding (1st–2nd gen)
  • Pirtobrutinib (non-covalent) active against C481S resistance mutations
  • Zanubrutinib FDA-approved now available as 160mg tablet — halving pill burden
  • BRUIN CLL-321 (Phase 3): pirtobrutinib vs idelalisib/rituximab in cBTKi-pretreated pts
  • Cardiac toxicity (AF, hypertension) remains a class concern with ibrutinib
Approved

BCL-2 Inhibitor + Combinations

Venetoclax ± Obinutuzumab · ± Acalabrutinib

  • CLL14 6-year data: venetoclax-obinutuzumab — durable remissions maintained
  • Venetoclax may neutralise adverse prognosis of short telomere length (CLL14)
  • AMPLIFY (Ph3): acalabrutinib + venetoclax — 35% PFS improvement vs chemoimmunotherapy
  • AbbVie sNDA submitted July 2025 for acalabrutinib + venetoclax combination
  • Fixed-duration all-oral doublets now the front-runner for treatment-naïve patients
Pipeline

BTK Degraders (PROTACs)

Bexobrutideg (NX-5948) · BGB-16673 · NX-2127

  • Induce BTK protein ubiquitination via cereblon E3 ligase → proteasomal degradation
  • Overcome C481S and other covalent BTKi resistance mutations
  • Bexobrutideg (NX-5948) Phase 1: ORR 80.9% in heavily pretreated R/R CLL
  • FDA Fast Track designation granted for NX-5948 (Jan 2024)
  • Early safety favorable: no new-onset AF/flutter reported in Phase 1 data
Emerging

Bispecific Antibodies

Epcoritamab (CD3×CD20) · Combinations under study

  • Subcutaneous CD3×CD20 T-cell engager; redirects cytotoxic T cells to CLL cells
  • EPCORE CLL-1 (Ph1b/2): promising efficacy in R/R CLL post-cBTKi
  • Combinations under investigation: epcoritamab + venetoclax; + pirtobrutinib
  • Potential for fixed-duration approaches without continuous oral therapy
  • Updated ICML 2025 data — activity confirmed in heavily pretreated patients
Emerging

CAR-T Cell Therapy

Liso-cel (CD19) · 3rd-gen CAR-T · CAR-NK

  • Liso-cel FDA approved March 2024 for R/R CLL/SLL (TRANSCEND-CLL-004)
  • TRANSCEND-CLL-004: CR rate 18% at higher dose; Grade 3 CRS 85%, neurotox 45%
  • 3rd-gen CAR-T (Phase 1): 6/9 pts achieved CR; 5/6 uMRD at 3 months post-infusion
  • CAR-NK: donor cord blood-derived; avoids manufacturing delay; under early study
  • Rapid CLL disease kinetics and bridging therapy availability remain challenges
Strategy

MRD-Guided Therapy

Ibrutinib + Venetoclax · FLAIR / CLL17 trials

  • MRD-directed ibrutinib + venetoclax significantly improved OS vs FCR chemoimmunotherapy
  • Treatment duration adapted to MRD status — minimizes exposure, avoids resistance
  • CLL17 trial: ibrutinib mono vs venetoclax-obinutuzumab vs ibrutinib-venetoclax
  • First head-to-head comparison of fixed-duration oral doublet vs antibody-based SOC
  • Anticipated to define whether oral doublets can replace antibody-containing regimens
2

Key Trial Highlights — 2024–2025


NX-5948-301 (Bexobrutideg) Phase 1a

BTK Degrader — R/R CLL

Heavily pretreated patients (median 4 prior lines) with BTK, BCL-2 and CAR-T exposure. No patient profile showed intrinsic resistance. Active irrespective of TP53, PLCG2, or BCL2 mutation status. No dose-limiting toxicities; no new-onset AF/flutter.

80.9%ORR (n=47)
97.9%prior cBTKi
83%prior BCL-2i
AMPLIFY Phase 3

Acalabrutinib + Venetoclax ± Obinutuzumab

Fixed-duration all-oral doublet vs chemoimmunotherapy in treatment-naïve CLL (excl. del17p/TP53 mut). 35% reduction in risk of progression or death over chemoimmunotherapy. sNDA submitted to FDA July 2025. Most common Grade ≥3 AE: neutropenia (26.8%).

HR 0.65PFS vs chemo-IT
p=0.004statistical significance
SEQUOIA (5-yr update) Phase 3

Zanubrutinib vs BR — Treatment-Naïve CLL

Five-year follow-up from ASH 2024 confirms sustained PFS benefit of zanubrutinib over bendamustine-rituximab. Tolerability and long-term safety profile reinforce zanubrutinib as preferred second-generation BTKi. Dose reduction to 160mg tablet approved in 2025, improving adherence in older patients.

5-yrsustained PFS benefit
160mgnew tablet formulation
EPCORE CLL-1 Phase 1b/2

Epcoritamab — R/R CLL Bispecific Data

Subcutaneous epcoritamab (CD3×CD20) in patients post ≥2 lines including cBTKi. Updated data at ICML 2025 confirmed durable clinical activity. Epcoritamab combinations with venetoclax and pirtobrutinib under active investigation as next-generation fixed-duration immunotherapy approaches.

SCsubcutaneous dosing
≥2prior lines required
3

Prognostic & Predictive Biomarkers


High-Risk / Adverse Markers

High Riskdel(17p) / TP53 mutation — shorter TTP with most targeted therapies; BTKi preferred over venetoclax-based upfront
High Riskdel(11q) — associated with lymphadenopathy and aggressive disease course
ResistanceBTK C481S mutation — primary covalent BTKi resistance; addressed by pirtobrutinib and BTK degraders
ResistancePLCG2 mutations — downstream BCR signalling bypass; associated with BTKi failure
ResistanceBCL-2 G101V mutation — venetoclax resistance; emerging challenge in relapsed disease
AdverseUnmutated IGHV — shorter time to first treatment; continuous BTKi preferred over fixed-duration in some models

Favourable / Predictive Markers

FavourableMutated IGHV — longer treatment-free intervals; may benefit most from fixed-duration venetoclax regimens
PredictiveuMRD (undetectable MRD) — strongest predictor of durable remission; now guides treatment duration in FLAIR/CLL17
Favourabledel(13q14) as sole abnormality — most favourable cytogenetic finding; longest OS and PFS
StagingRai / Binet staging — clinical staging using lymphocyte counts, organomegaly, haemoglobin and platelets; guides watch-and-wait decisions
MonitorCD38 / ZAP-70 — surrogate IGHV mutation markers; less routinely used since direct IGHV sequencing became standard
EmergingTelomere length — short telomeres historically adverse; CLL14 data suggests venetoclax may neutralise this risk
4

Current Clinical Challenges


The Double-Refractory Patient

Patients refractory to both BTKi and venetoclax (BCL-2i) represent the most urgent unmet need in CLL. Prognosis is very poor. No standard approach exists — these patients require enrolment in clinical trials evaluating BTK degraders, bispecifics, CAR-T, and novel combinations.

Optimal Therapy Sequencing

With multiple effective agents, the order of BTKi → BCL-2i vs BCL-2i → BTKi profoundly affects resistance profiles. Cross-resistance patterns differ and remain under active study. The ReVenG trial is exploring venetoclax retreatment after first-line venetoclax-based therapy.

Fixed-Duration vs Continuous Therapy

Fixed-duration regimens offer cost savings, resistance avoidance, and treatment-free time — but continuous BTKi therapy may provide superior MRD suppression in unmutated IGHV. CLL17 will provide the first direct head-to-head comparison to resolve this debate.

BTKi Toxicity Management

Ibrutinib-related atrial fibrillation, hypertension, and bleeding complicate long-term use. Zanubrutinib and acalabrutinib offer improved selectivity. Dose-modification strategies and multidisciplinary cardiovascular co-management are essential in older, comorbid patients.

Clonal Evolution & Resistance

Sequential therapy drives genomic evolution — acquisition of BTK C481S, PLCG2, and BCL-2 G101V resistance mutations. Whole-genome sequencing and liquid biopsy (ctDNA) are increasingly used to track clonal dynamics and guide treatment switches early.

Adherence & Access

Long-term oral therapy in an elderly, comorbid population (median age 70) presents adherence challenges. Pill burden, drug interactions, and financial toxicity affect real-world outcomes. The zanubrutinib 160mg tablet approval addresses pill burden directly.

5

Clinical Treatment Pathway — 2025 Framework


Stratified Management by Setting & Risk

1st Line

Fit patients without del(17p)/TP53 mut: Fixed-duration venetoclax + obinutuzumab (CLL14) or venetoclax + acalabrutinib (AMPLIFY, pending approval); alternatively continuous zanubrutinib or acalabrutinib monotherapy. Mutated IGHV may favor venetoclax-based fixed-duration; unmutated IGHV may favor continuous BTKi.

1st Line

del(17p) / TP53 mutant CLL: Continuous BTKi (zanubrutinib or acalabrutinib) — standard of care. Venetoclax ± antibody is an option. Avoid chemoimmunotherapy. High-risk patients may be considered for clinical trials of upfront combination strategies.

Relapsed

Post-BTKi relapse: Venetoclax + rituximab or obinutuzumab (if BCL-2i naïve). Pirtobrutinib if cBTKi failure but BCL-2i naïve. Consider MRD-guided retreat strategies (ReVenG trial data emerging for venetoclax retreatment).

Relapsed

Post-venetoclax relapse: BTKi or pirtobrutinib (if BTKi naïve). Epcoritamab (bispecific antibody) is emerging as an option post-cBTKi; CAR-T cell therapy (liso-cel) now FDA approved in R/R CLL/SLL post-BTKi and BCL-2i.

Double-Refractory

Post-BTKi + Post-BCL-2i: Enrol in clinical trial as priority. Investigational options: BTK degraders (NX-5948, BGB-16673 Phase 1 data encouraging), bispecific antibodies, CAR-T + ibrutinib combinations, novel BCL-2 inhibitors. No established standard outside trials.

The 2025 Bottom Line

CLL treatment is at an inflection point. Fixed-duration oral doublets (BTKi + venetoclax) are rapidly becoming the new standard of care, offering deep remissions with treatment-free intervals. The next frontier is the double-refractory patient — where BTK degraders, bispecific antibodies, and next-generation CAR-T therapies offer genuine therapeutic hope for the first time.

The integration of MRD as a treatment endpoint — rather than a prognostic marker — marks a paradigm shift. Therapy will increasingly be individualised by IGHV status, cytogenetic risk, MRD kinetics, and comorbidity profile. The era of one-size-fits-all CLL management is ending.

Key trials to watch: CLL17, FLAIR extension, NX-5948-301 Phase 1b/2 expansion, BRUIN CLL-321, and ongoing bispecific combination studies at ASH 2025 and beyond.

mitotics.com · Molecular Oncology Clinical Insights · 2025