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CTLA-4 inhibition

CompoundTremelimumab

Area under investigation

Advanced solid tumors, uHCC, Metastatic urothelial carcinoma, Muscle-invasive bladder cancer, NSCLC, SCLC

Scientific PillarImmuno-Oncology

Target Overview

Cytotoxic T–lymphocyte-associated protein 4 (CTLA-4) is expressed exclusively on the surface of T cells.1 CTLA-4 serves to inhibit T-cell activation through delivery of inhibitory signals and through ligand competition with the costimulatory receptor, cluster of differentiation 28 (CD28).1,2

Inhibition of CTLA-4 can shift the balance of signaling in the immune system in favor of greater T-cell activation, engendering a greater immune response and potentially resulting in the rejection of tumor by the host’s immune system.2

Compound Overview

Tremelimumab is an anti-CTLA-4 mAb that is being clinically evaluated in combination with durvalumab, a programmed cell death ligand-1 (PD-L1) inhibitor, for the potential treatment of cancer.

Mechanism of Action

  • Mechanism of Action
  • Mechanism of Action

Figures adapted from MedImmune Oncology Pipeline: Tremelimumab, targeting CTLA-4. ©2013 MedImmune, LLC. 11326A. AstraZeneca; 264701, May 2013.

References

1. Pardoll DM. Nat Rev Cancer. 2012;12(4):252-264. 2. Wolchok JD, Saenger Y. Oncologist. 2008;13(suppl 4):2-9.

Clinical trial information


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Abbreviations

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  • 1L

    first line

  • 3L

    third line

  • ADA

    anti-drug antibody

  • AE

    adverse event

  • AESI

    adverse event of special interest

  • ALK

    anaplastic lymphoma kinase

  • APF12

    alive and progression-free survival at 12 months

  • BCLC

    Barcelona Clinic Liver Cancer

  • BICR

    blinded independent central review

  • BOR

    best overall response

  • CD28

    cluster of differentiation 28

  • CD80

    cluster of differentiation 80

  • CD86

    cluster of differentiation 86

  • CNS

    central nervous system

  • CRT

    chemoradiotherapy

  • CT

    chemotherapy

  • cTACE

    conventional transarterial chemoembolization

  • CTLA-4

    cytotoxic T–lymphocyte-associated antigen 4

  • D

    durvalumab

  • DCR

    disease control rate

  • DEB-TACE

    drug-eluting bead-TACE

  • DFS

    disease-free survival

  • DoR

    duration of response

  • DoT

    duration of treatment

  • ECOG PS

    Eastern Cooperative Oncology Group Performance Score

  • EFS

    event-free survival

  • EGFR

    epidermal growth factor receptor

  • EGFRm

    epidermal growth factor receptor mutation

  • EORTC QLQ-C30

    European Organization for the Research and Treatment of Cancer Quality of Life Questionnaire

  • EP

    carboplatin or cisplatin + etoposide

  • ES-SCLC

    extensive stage small-cell lung cancer

  • EV

    enfortumab vedotin

  • FACT-BL

    functional assessment of cancer therapy-bladder

  • GI

    gastrointestinal

  • HBV

    hepatitis B virus

  • HCC

    hepatocellular carcinoma

  • HCV

    hepatitis C virus

  • HDV

    hepatitis D virus

  • HNSCC

    head and neck squamous cell carcinoma

  • HRQoL

    health-related quality of life

  • imAEs

    immune-mediated adverse events

  • IMP

    investigational medicinal product

  • IV

    intravenous

  • KEAP1

    Kelch-like ECH-associated protein 1

  • KRAS

    Kirsten rat sarcoma viral oncogene homolog

  • LRT

    locoregional treatment

  • LS-SCLC

    limited-stage small cell lung cancer

  • mAb

    monoclonal antibody

  • MHC

    major histocompatibility complex

  • MIBC

    muscle invasive bladder cancer

  • MOA

    mechanism of action

  • mRECIST

    modified Response Evaluation Criteria in Solid Tumors

  • MRI

    magnetic resonance imaging

  • NSCLC

    non-small cell lung cancer

  • ORR

    overall or objective response rate

  • OS

    overall survival

  • OS-12

    overall survival at 12 months

  • OS-24

    overall survival at 24 months

  • PCI

    prophylactic cranial irradiation

  • pCR

    pathological complete response

  • PD

    progressive disease

  • PD-L1

    programmed cell death ligand-1

  • pDS

    pathologic downstaging

  • PFS

    progression-free survival

  • PFS-12

    progression-free survival at 12 months

  • PFS-18

    progression-free survival at 18 months

  • PFS2

    time to second progression or death

  • PK

    pharmacokinetics

  • PRAEs

    possibly related to treatment adverse events

  • PRO

    patient-reported outcomes

  • PtCh

    platinum-based chemotherapy

  • PVT

    portal vein thrombosis

  • PVTT

    portal vein tumor thrombosis

  • Q*W

    every * weeks

  • Q3W

    every 3 weeks

  • Q4W

    every 4 weeks

  • QD

    once daily

  • R

    randomization

  • RECIST

    Response Evaluation Criteria in Solid Tumors

  • RECIST v1.1

    Response Evaluation Criteria in Solid Tumors version 1.1

  • RNA

    ribonucleic acid

  • SAE

    serious adverse event

  • SCLC

    small cell lung cancer

  • SoC

    standard of care

  • STK11

    serine/threonine kinase 11

  • STRIDE

    Single Tremelimumab Regular Interval Durvalumab

  • T

    tremelimumab

  • TACE

    transarterial chemoembolization

  • TC

    tumor cell

  • TCC

    transitional cell carcinoma

  • TCR

    T-cell receptor

  • TFST

    time to first subsequent therapy

  • TIGIT

    T-cell immunoreceptor with immunoglobulin and ITIM domains

  • TMB

    tumor mutation burden

  • TNM

    tumor node metastasis staging

  • TTP

    time to progression

  • UC

    urothelial cancer

  • uHCC

    unresectable hepatocellular carcinoma

  • Vp3

    first-order branch of the portal vein

  • Vp4

    main trunk of the portal vein or contralateral first-order branch

  • WHO

    World Health Organization

Some compounds herein refer to selected AstraZeneca pipeline products still under development. AstraZeneca pipeline products are investigational products and, as such, are not approved by the US Food & Drug Administration (FDA), the European Medicines Agency (EMA) or any other regulatory agency for the uses under investigation. Information regarding these investigational products should, under no circumstances, be regarded as a recommendation for their use or of their safety or efficacy.

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Veeva ID: Z4-80919 US-109129 DE-92568 Last Updated April 20263/26
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