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Curative therapies for sickle cell disease

Matt Hsieh, MD

March 2025

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Disclosures

  • none

  • off label use of medications for hematopoietic cell transplantation include: cyclophosphamide, fludarabine, alemtuzumab, abatacept

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Objectives

  • recognize recently approved medications for sickle cell include L-glutamine (Endari), crizanlizumab (Adakveo)
  • discuss matched related donor HCT results in ablative and non-ablative regimens
  • discuss haplo HCT results using post transplant cyclophosphamide (PTCy) and T cell depletion based regimens
  • recognize recently approved autologous gene therapies include Lyfgenia (adding normal beta-globin; lovotibeglogene or lovo-cel) and Casgevy (reactivating fetal hemoglobin; exagamglogene or exa-cel)

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Sickle cell is caused by a genetic mutation

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Acute and chronic sickle manifestations

Thein, Blood 2019

Cardinal features of SCD:

Anemia*

Hemolysis*

Pain crises*

Acute chest syndrome*

*reversible by hematopoietic

cell transplant (HCT)

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Tisdale, Science 2020

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Approved medications for SCD

  • hydroxyurea: reactivate fetal hemoglobin (HbF) and reduce WBC
    • increase HbF and total hemoglobin levels
    • disease modifying medication
  • L-glutamine: anti-oxidant like properties, prolong red cell survival
    • no change in CBC, hemolysis labs
  • voxelotor: increase oxygen binding to reduce sickle polymerization
    • higher hgb
    • recently withdrawn due to higher rates of VOC and possibly deaths
  • crizanlizumab: p-selectin inhibitor, reduce red cell and plts adhering to blood vessel endothelium
    • no change in CBC, hemolysis labs
  • mitapivat (in clinical trials): pyruvate kinase activator, prolong red cell survival
    • higher hgb
  • other anti-sickling medication in various stages of development and clinical trials

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HbSS

    • HbS 90%
    • HbF <2%
    • Hgb 6-7

HbSS on HU

    • HbS 70%
    • HbF 20-30%
    • Hgb 7-9

HbSS on voxelotor (off market)

    • HbS 90%
    • HbF <5%
    • Hgb 8

HbSS on L-glutamine

    • HbS 90%
    • HbF <5%
    • Hgb 7

HbSS on crizanlizumab

    • HbS 90%
    • HbF <5%
    • Hgb 7

Key hematologic results with life-long compliance in taking medication

Modestly

reduce pain crisis

reduce hospitalization

Significantly

reduce pain crisis

reduce hospitalization

Higher hgb

(withdrawn due to higher rates of VOC and possibly death)

Modestly

reduce pain

Fewer patients derive clinical benefits

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HCT for SCD: matched related donors

  • leukemia type conditioning regimen, myeloablative
    • chemotherapy based (high intensity) 🡪 aiming for full replacement of marrow by donor cells (full donor chimerism)
    • occasionally, as low as 10% donor chimerism still had hematologic benefit
    • all in children and young adults (<25 yo)
  • for older adults (>25 yo) or those with compromised heart, lung, liver, or renal function, non-ablative regimen
    • antibody and low dose radiation based (low intensity)
    • mixed chimerism (5-95% donor) was much more common

Walters et al, 2001; Bernaudin et al, 2008

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Examples of conditioning regimens for matched related donor HCT

-7

-6

-5

-4

-3

-2

-1

0

-8

Sirolimus

TBI 300 cGy

Unmanipulated G-CSF mobilized PBSC infusion

Alemtuzumab (1 mg/kg total)

-9

-10

Rabbit ATG (20 mg/kg total)

Busulfan 16mg/kg total

Cyclophos 200 mg/kg total

Unmanipulated BM infusion

Cyclosporine + methotrexate

“Bu4-Cy4-rATG” – myeloablative (high intensity)

“Alem-300 TBI” – non-myeloablative (low intensity)

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Transplant outcomes

Alem-300 cGy TBI

Bu4-Cy4-rATG

Overall survival

93%

96%

Graft failure (sickle recurrence)

13%

2%

GVHD

2% aGVH

0% cGVH

15% aGVH

15% cGVH

Mixed chimerism (5-95% donor)

90%

20%

CMV requiring treatment

13%

24%

EBV requiring treatment

3%

2.6%

BK, hemorrhagic cystitis

0

7%

Veno-occlusive disease (sinusoidal obstructive disease)

0

1%

Alzahrani M, BJH 2020; Bernaudin F, Haematologica 2019

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Comparing nonablative vs ablative, MRD

  • non-ablative (low intensity) regimen, e.g. alem-300 TBI
    • applicable to patients with compromised organ function (cirrhosis, pulm HTN, or dialysis)
    • stable lung, liver, kidney function post HCT
    • low intensity 🡪 likely more fertility preservation
  • ablative (high intensity), e.g. Bu4-Cy4-rATG
    • typically for children and young adults
    • in pre-pubertal children, spontaneous puberty observed post HCT
    • although requires normal function pre-HCT, lung, liver, and kidney functions also remain stable post HCT

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Initial report with improved haplo HCT with PTCy

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Haplo HCT, 2 broad categories

  • the survival and success rates of haplo HCT have steadily improved
  • there are many haplo conditioning regimens. They can be grouped
  • post-transplant cyclophosphamide (PTCy)
    • giving Cy after donor cell infusion 🡪 reduces total pool of donor lymph and expand Treg 🡪 reduce GvHD
    • moderately high intensity
    • sickle free survival >80%, aGVHD ranged from 0 to 25%
  • ex vivo T depletion
    • reduce the activated T cells in the donor cell graft 🡪 reduce GvHD
    • moderately high intensity
    • sickle free survival >80%, aGVHD ranged from 6 to ~30%

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When an antigen presenting cell shows a ‘foreign’ antigen to T cell receptor (TCR), this activates signal 1 of the T cell activation cascade.

There are several other co-stimulatory signals (also known as signal 2) that further elaborate the T cell activation process.

Danese S et al, Gut, 2003

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Ongoing improvements in haplo HCT

  • better supportive care, antimicrobial prophylaxis
  • thoughtful design of conditioning regimen (PT-Cy, T cell depletion)
  • during pre-HCT testing, when recipient antibody to antigen on donor cells is detected (positive donor specific antibody)
    • many chemo and antibody combo to reduce DSA
    • improve engraftment
  • co-stimulatory blockade
    • Co-stimulatory signal is the second part of the T cell activation process. Blocking this step improves both engraftment and reduces GvHD
    • Ngwube A et al, Blood Adv 2020; Jaiswal SR et al, BBMT 2020

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AUTOLOGOUS gene manipulation

  • for MANY patients, there are no suitable matched related donors, but they have disease severe enough to consider a transplant
  • their curative options are haplo vs auto gene therapy
  • gene manipulation = gene therapy (general term)
    • Gene addition: add one or more correct copies of the normal beta-globin gene (lovotibeglogene or lovo-cel, Lyfgenia)
    • Gene edit: change an existing gene to alter production. There has been several studies to increase HbF production (exagamglogene or exa-cel, Casgevy)
    • Gene correction: fix the actual sickle mutation in the beta-globin gene. Clinical trials planned

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Hematologic improvement after gene ADDition

J Kanter et al, NEJM 2022

ε

δ

βs

β T87Q

FDA approved in 2023, Lyfgenia

1

  • lentiviral vector
  • insert a normal beta-globin gene, modified to have additional anti-sickling property
  • expression of T87Q sufficient to counter HbS 🡪 similar to sickle trait
  • increase in total hgb, reduce VOC and hosp adm

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Hematologic improvement after gene EDIT

ε

δ

βs

H Frangoul et al, NEJM 2024

FDA approved in 2023, Casgevy

erythroid

enhancer

BCL11A

1

CRISPR cut

2

Reduce expression

3

Reactivate gamma-globin expression

Chr 2

Chr 11

  • high HbF dilutes HbS to reduce sickle polymerization
  • similar to taking HU
  • increase total hgb, reduce VOC and hosp adm

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matched related HCT vs gene therapy vs haplo HCT?

FIRST CHOICE: matched related HCT

- longer history and more experience

- side effects, complications, success/failure rates are well known

  • many transplant centers already offer this option
  • age <30 and no comorbid conditions 🡪 ablative or reduced toxicity to aim full donor chimerism
  • presence of comorbid condition 🡪 low intensity regimen

SECOND CHOICE:

- although haplo = gene therapy, haplo is more prob accessible

- increasingly more transplant centers are offering haplo

  • gene therapy more expensive (for now)
  • sequence of treatment matters
    • Gene therapy first, if unsuccessful, can salvage with haplo
    • But if haplo first and unsuccessful, cannot salvage with gene therapy

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HbSS (no tx)

    • HbS 90%
    • HbF <2%
    • Hgb 6-7

HbSS on HU

    • HbS 70%
    • HbF 20-30%
    • Hgb 7-9

HbSS on exchange

    • HbS 20-50%
    • HbA 40-70%
    • Hgb 8-10

HbSS, gene therapy

    • HbS 50+%
    • HbA* 40-50% or
    • HbF 20-40%
    • Hgb 10-11

HbAS donor

    • HbS 40%
    • HbA 55%
    • Hgb 11-13

HbAA donor

    • HbS 0%
    • HbA 95%
    • Hgb 11-13

Life-long compliance in taking meds

One-time, intensive treatment

Every 4-6 weeks

Comparing key hematologic outcomes after various therapies