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ERα degradation and antagonism

CompoundCamizestrant

Area under investigation

Advanced solid tumors, HR-positive/HER2-negative breast cancer

Scientific PillarTumor Drivers & Resistance Mechanisms

Target Overview

Estrogen receptor alpha (ERα) is expressed in about 70% of breast cancer cases.1 ERα activity is essential for ER+ breast cancers, and while they may respond well to anti-estrogen therapies, such as aromatase inhibitors (AIs) and selective estrogen receptor modulators (SERMs),2 resistance can emerge.3

Selective estrogen receptor degraders (SERDs) antagonize ERα and target it for degradation.1

Compound Overview

Camizestrant is an investigational next generation, oral, nonsteroidal ERα antagonist and selective estrogen receptor degrader. The molecule is being clinically evaluated as a potential treatment for HR+, HER2- breast cancers.

Mechanism of Action

  • Mechanism of Action

Bidard FC et al. Poster presented at: San Antonio Breast Cancer Symposium (SABCS); December 7-10, 2021; San Antonio, TX.

References

1. Gombos A. Curr Opin Oncol. 2019;31(5):424-429. 2. Early Breast Cancer Trialists’ Collaborative Group (EBCTCG). Lancet. 2005;365(9472):1687-1717. 3. Jeselsohn R, Buchwalter G, De Angelis C, et al. Nat Rev Clin Oncol. 2015;12(10):573-583.

Target Overview

Estrogen receptor alpha (ERα) is expressed in about 70% of breast cancer cases.1 ERα activity is essential for ER+ breast cancers, and while they may respond well to anti-estrogen therapies, such as aromatase inhibitors (AIs) and selective estrogen receptor modulators (SERMs),2 resistance can emerge.3

Selective estrogen receptor degraders (SERDs) antagonize ERα and target it for degradation.1

Compound Overview

Camizestrant is an investigational next generation, oral, nonsteroidal ERα antagonist and selective estrogen receptor degrader. The molecule is being clinically evaluated as a potential treatment for HR+, HER2- breast cancers.

Mechanism of Action

  • Mechanism of Action

Bidard FC et al. Poster presented at: San Antonio Breast Cancer Symposium (SABCS); December 7-10, 2021; San Antonio, TX.

References

1. Gombos A. Curr Opin Oncol. 2019;31(5):424-429. 2. Early Breast Cancer Trialists’ Collaborative Group (EBCTCG). Lancet. 2005;365(9472):1687-1717. 3. Jeselsohn R, Buchwalter G, De Angelis C, et al. Nat Rev Clin Oncol. 2015;12(10):573-583.

Clinical trial information


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Area under investigation=true,Advanced solid tumors,HR-positive/HER2-negative breast cancer

CAMBRIA-1 trial overview

Tumor

HR+/HER2- eBC with intermediate/high risk for disease recurrence and post definitive locoregional therapy and adjuvant ET for ≥2 and up to 5 years

Trial Identifier

NCT05774951

Phase

III

Regimen

Camizestrant; standard endocrine therapy of investigator's choice (aromatase inhibitors or tamoxifen)

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CAMBRIA-2 trial overview

Tumor

HR+/HER2- eBC with intermediate-high or high risk for disease recurrence after completion of definitive locoregional therapy (with or without chemotherapy)

Trial Identifier

NCT05952557

Phase

III

Regimen

Camizestrant ± abemaciclib; standard endocrine therapy of investigator's choice ± abemaciclib

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CYCAD-1 trial overview

Tumor

HR+/HER2- advanced breast cancer, metastatic high-grade serous ovarian cancer

Trial Identifier

NCT06188520

Phase

I/IIa

Regimen

AZD8421; AZD8421 + camizestrant + abemaciclib; AZD8421 + camizestrant + ribociclib; AZD8421 + camizestrant + palbociclib

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EvoPAR-Breast01 trial overview

Tumor

Advanced HR+/HER2- breast cancer with germline or somatic mutations in BRCA1/2 or PALB2 genes

Trial Identifier

NCT06380751

Phase

III

Regimen

Saruparib + camizestrant; physician’s choice CDK4/6i + physician’s choice endocrine therapy; physician’s choice CDK4/6i + camizestrant

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PETRA trial overview

Tumor

Advanced solid tumors (advanced/metastatic ovarian cancer, HR+/HER2- breast cancer, TNBC, pancreatic cancer, prostate cancer, NSCLC, SCLC, gastric cancer, biliary cancer, cervical cancer, endometrial cancer, CRC, bladder cancer)

Trial Identifier

NCT04644068

Phase

I/IIa

Regimen

Saruparib; saruparib + paclitaxel; saruparib + carboplatin ± paclitaxel; saruparib + T-DXd; saruparib + Dato-DXd; saruparib + camizestrant

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fam-trastuzumab deruxtecan-nxki in US only; trastuzumab deruxtecan in other regions of world.

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SERENA-4 trial overview

Tumor

HR+/HER2- advanced/metastatic breast cancer, 1L

Trial Identifier

NCT04711252

Phase

III

Regimen

Camizestrant + palbociclib; anastrozole + palbociclib

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Abbreviations

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  • 1L

    first line

  • aBC

    advanced breast cancer (locally advanced [inoperable] or metastatic breast cancer)

  • AE

    adverse event

  • AI

    aromatase inhibitor

  • BC

    breast cancer

  • CBR

    clinical benefit rate

  • CBR24

    clinical benefit rate at 24 weeks

  • CDK4/6i

    cyclin-dependent kinase 4/6 inhibitor

  • CTCAE

    Common Terminology Criteria for Adverse Events

  • ctDNA

    circulating tumor DNA

  • DoR

    duration of response

  • DRFS

    distant relapse-free survival

  • eBC

    early breast cancer

  • ECOG PS

    Eastern Cooperative Oncology Group Performance Score

  • ER

    estrogen receptor

  • ER+

    estrogen receptor positive

  • ERE

    estrogen response element

  • ERα

    estrogen receptor alpha

  • ESR1

    estrogen receptor 1

  • ESR1m

    estrogen receptor 1 mutation

  • ET

    endocrine therapy

  • HBV

    hepatitis B virus

  • HCV

    hepatitis C virus

  • HER2

    human epidermal growth factor receptor 2

  • HER2-

    human epidermal growth factor receptor 2 negative

  • HR

    hormone receptor

  • HRQoL

    health-related quality of life

  • IBCFS

    invasive breast cancer-free survival

  • LHRH

    luteinizing hormone-releasing hormone

  • MRI

    magnetic resonance imaging

  • OD

    once daily

  • OFS

    ovarian function suppression

  • ORR

    overall or objective response rate

  • OS

    overall survival

  • pCR

    pathological complete response

  • PFS

    progression-free survival

  • PFS2

    time to second progression or death

  • PK

    pharmacokinetics

  • PRO

    patient-reported outcomes

  • QoL

    quality of life

  • R

    randomization

  • RECIST

    Response Evaluation Criteria in Solid Tumors

  • SAE

    serious adverse event

  • SERD

    selective estrogen receptor degrader

  • SERM

    selective estrogen receptor modulator

  • SoC

    standard of care

  • TEAE

    treatment emergent adverse event

  • TFST

    time to first subsequent therapy

  • TSST

    time to start of second subsequent therapy

  • TTC

    time to chemotherapy

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: Z4-84958 US-109129 DE-92568 Last Updated October 20263/26
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