Camizestrant

Summary

Camizestrant (CHEMBL4650365) is a phase-3 clinical-stage small molecule targeting ESR1; indicated across 3 conditions including breast neoplasm and liver disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (ESR1)
• Indications: 3 conditions
• Clinical trials: 19
• Chemistry: 476.5 Da · C24H28F4N6

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4650365
Name	Camizestrant
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	134453496
Molecular formula	C24H28F4N6
Molecular weight	476.5
InChIKey	WDHOIABIERMLGY-CMJOXMDJSA-N

SMILES: C[C@@H]1CC2=C(C=CC3=C2C=NN3)[C@H](N1CC(F)(F)F)C4=NC=C(C=C4)NC5CN(C5)CCCF

IUPAC name: N-[1-(3-fluoropropyl)azetidin-3-yl]-6-[(6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-3,6,8,9-tetrahydropyrazolo[4,5-f]isoquinolin-6-yl]pyridin-3-amine

Also known as: AZ-14066724, AZ14066724, AZD-9833, Azd9833, AZD9833, Camizestrant, CPD 28, CAMIZESTRANT, ESTROGEN RECEPTOR ANTAGONIST 2, CAMIZESTRANT (AZD9833)

Patent coverage: 199 distinct patent families (504 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 443 (88%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
ESR1	Estrogen receptor-α	Antagonist	9.8	1.7%	P03372

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Estrogen receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Histamine H3 receptor, Cytochrome P450 2D6, Cytochrome P450 3A4.

Bioactivity

ChEMBL activities: 22 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ESR1	9.92	IC50	0.12	nM	CHEMBL_ACT_27018827
ESR1	9.9	IC50	0.13	nM	CHEMBL_ACT_22429831
ESR1	9.8	IC50	0.16	nM	CHEMBL_ACT_22429833
ESR1	9.8	IC50	0.16	nM	CHEMBL_ACT_22430102
ESR1	9.8	IC50	0.16	nM	CHEMBL_ACT_22902435
ESR1	9.77	IC50	0.17	nM	CHEMBL_ACT_27018821
ESR1	9.08	IC50	0.84	nM	CHEMBL_ACT_29106419
ESR1	8.82	IC50	1.5	nM	CHEMBL_ACT_27018818
KCNH2	8.82	IC50	1.5	nM	CHEMBL_ACT_27918962
ESR1	8.82	IC50	1.5	nM	CHEMBL_ACT_28295987
ESR1	8.74	IC50	1.8	nM	CHEMBL_ACT_27018824
KCNH2	8.74	IC50	1.8	nM	CHEMBL_ACT_27918965
ESR1	8.74	IC50	1.8	nM	CHEMBL_ACT_28295990
KCNH2	8.68	IC50	2.1	nM	CHEMBL_ACT_27918953
KCNH2	8.62	IC50	2.4	nM	CHEMBL_ACT_27918908
ESR1	8.62	IC50	2.4	nM	CHEMBL_ACT_28295933
ESR1	8.6	IC50	2.51	nM	CHEMBL_ACT_22430138
ESR1	8.6	IC50	2.51	nM	CHEMBL_ACT_22902423
ESR1	8.2	IC50	6.31	nM	CHEMBL_ACT_22429830
HRH3	6.48	IC50	330	nM	CHEMBL_ACT_22429835
CYP3A4	5.66	IC50	2200	nM	CHEMBL_ACT_22429868
CYP2D6	5.37	IC50	4300	nM	CHEMBL_ACT_22429870

Target pathways

Aggregated over 1 target gene(s): ESR1.

Top Reactome pathways

17 total, by targets touching each:

Pathway	Targets	Genes
Nuclear signaling by ERBB4	1	ESR1
PIP3 activates AKT signaling	1	ESR1
Constitutive Signaling by Aberrant PI3K in Cancer	1	ESR1
Nuclear Receptor transcription pathway	1	ESR1
SUMOylation of intracellular receptors	1	ESR1
Ovarian tumor domain proteases	1	ESR1
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	1	ESR1
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors	1	ESR1
RUNX1 regulates estrogen receptor mediated transcription	1	ESR1
ESR-mediated signaling	1	ESR1
RUNX1 regulates transcription of genes involved in WNT signaling	1	ESR1
Regulation of RUNX2 expression and activity	1	ESR1
Extra-nuclear estrogen signaling	1	ESR1
Estrogen-dependent gene expression	1	ESR1
Mitochondrial unfolded protein response (UPRmt)	1	ESR1
Developmental Lineage of Mammary Gland Luminal Epithelial Cells	1	ESR1
Developmental Lineage of Mammary Gland Alveolar Cells	1	ESR1

Dominant GO biological processes

GO term	Targets
negative regulation of transcription by RNA polymerase II	1
antral ovarian follicle growth	1
epithelial cell development	1
chromatin remodeling	1
regulation of DNA-templated transcription	1
regulation of transcription by RNA polymerase II	1
signal transduction	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
androgen metabolic process	1
male gonad development	1
negative regulation of gene expression	1
nuclear receptor-mediated steroid hormone signaling pathway	1
estrogen receptor signaling pathway	1
response to estradiol	1

Indications & clinical

Indications

3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
breast neoplasm	3	MONDO:0021100	MONDO:0007254
liver disorder	1	MONDO:0005154	EFO:0001421

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 19.

Phase distribution

Phase	Trials
PHASE1	8
PHASE3	5
PHASE2	4
PHASE1/PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04711252	PHASE3	ACTIVE_NOT_RECRUITING	A Comparative Study of AZD9833 Plus Palbociclib Versus Anastrozole Plus Palbociclib in Patients With ER-Positive HER2 Negative Breast Cancer Who Have Not Received Any Systemic Treatment for Advanced Disease
NCT04964934	PHASE3	ACTIVE_NOT_RECRUITING	Phase III Study to Assess AZD9833+ CDK4/6 Inhibitor in HR+/HER2-MBC With Detectable ESR1m Before Progression (SERENA-6)
NCT05774951	PHASE3	RECRUITING	A Study of Camizestrant in ER+/HER2- Early Breast Cancer After at Least 2 Years of Standard Adjuvant Endocrine Therapy
NCT05952557	PHASE3	RECRUITING	An Adjuvant Endocrine-based Therapy Study of Camizestrant (AZD9833) in ER+/HER2- Early Breast Cancer (CAMBRIA-2)
NCT06380751	PHASE3	RECRUITING	Saruparib (AZD5305) Plus Camizestrant Compared With CDK4/6 Inhibitor Plus Endocrine Therapy or Plus Camizestrant in HR-Positive, HER2-Negative (IHC 0, 1+, 2+/ ISH Non-amplified), BRCA1, BRCA2, or PALB2m Advanced Breast Cancer
NCT04214288	PHASE2	ACTIVE_NOT_RECRUITING	A Study to Investigate Efficacy and Safety With Oral AZD9833 Compared With Intramuscular Fulvestrant in Post-menopausal Women at Least 18 Years of Age With Advanced ER-positive HER2 Negative Breast Cancer
NCT04644068	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Study of AZD5305 as Monotherapy and in Combination With Anti-cancer Agents in Patients With Advanced Solid Malignancies
NCT06188520	PHASE1/PHASE2	RECRUITING	A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors
NCT07195227	PHASE2	RECRUITING	Efficacy and Safety of Camizestrant Plus Ribociclib in Patients With Breast Cancer
NCT07427394	PHASE2	RECRUITING	Study to Evaluate the Safety and Tolerability of Camizestrant in Combination With Atirmociclib in Women With Advanced Breast Cancer
NCT04588298	PHASE2	COMPLETED	A Study to Investigate the Biological Effects of AZD9833 in Women With ER-positive, HER2 Negative Primary Breast Cancer
NCT03616587	PHASE1	ACTIVE_NOT_RECRUITING	Study of AZD9833 Alone or in Combination in Women With Advanced Breast Cancer.
NCT04541433	PHASE1	COMPLETED	A Phase 1 Study of AZD9833 in Japanese Women With ER Positive, HER2 Negative Advanced Breast Cancer
NCT04546347	PHASE1	COMPLETED	A Study to Assess the Rel Bioavailability, Food Effect and Absolute Bioavailability on the Pharmacokinetics of AZD9833
NCT04818632	PHASE1	COMPLETED	AZD9833 China PK Study
NCT05438303	PHASE1	COMPLETED	Study to Assess the Effect of Co-Administration of AZD9833 on the Pharmacokinetics of Midazolam, of Omeprazole, of Celecoxib and of Dabigatran Etexilate in Healthy Postmenopausal Female Volunteers
NCT05551897	PHASE1	COMPLETED	A Study to Assess the Pharmacokinetics of Camizestrant (AZD9833) When Administered Alone and in Combination With Itraconazole
NCT05790304	PHASE1	COMPLETED	Study to Investigate Hepatic Impairment on PK, Safety, Tolerability of Camizestrant in Post-Menopausal Female Subjects
NCT06547164	PHASE1	COMPLETED	A Study to Investigate the Pharmacokinetics of Midazolam After Repeated Doses of Camizestrant (AZD9833) and to Investigate the Pharmacokinetics of Camizestrant When Administered Alone and in Combination With Carbamazepine in Healthy Post-Menopausal Female Participants

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

173 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
FULVESTRANT	ChEMBL + PubChem	Phase 4 (approved)	ESR1
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	ESR1
ALECTINIB	ChEMBL	Phase 4 (approved)	ESR1
APOMORPHINE	ChEMBL	Phase 4 (approved)	ESR1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ESR1
ASPIRIN	ChEMBL	Phase 4 (approved)	ESR1
AZTREONAM	ChEMBL	Phase 4 (approved)	ESR1
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	ESR1
BELINOSTAT	ChEMBL	Phase 4 (approved)	ESR1
BENZBROMARONE	ChEMBL	Phase 4 (approved)	ESR1
BEXAROTENE	ChEMBL	Phase 4 (approved)	ESR1
BISACODYL	ChEMBL	Phase 4 (approved)	ESR1
BITHIONOL	ChEMBL	Phase 4 (approved)	ESR1
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ESR1
BUTOCONAZOLE	ChEMBL	Phase 4 (approved)	ESR1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	ESR1
CASPOFUNGIN	ChEMBL	Phase 4 (approved)	ESR1
CEFADROXIL	ChEMBL	Phase 4 (approved)	ESR1
CEFEPIME	ChEMBL	Phase 4 (approved)	ESR1
CEFTAZIDIME	ChEMBL	Phase 4 (approved)	ESR1
CERIVASTATIN	ChEMBL	Phase 4 (approved)	ESR1
CHLOROTRIANISENE	ChEMBL	Phase 4 (approved)	ESR1
CISPLATIN	ChEMBL	Phase 4 (approved)	ESR1
CLOFAZIMINE	ChEMBL	Phase 4 (approved)	ESR1
CLOMIPHENE	ChEMBL	Phase 4 (approved)	ESR1
CYCLOFENIL	ChEMBL	Phase 4 (approved)	ESR1
DANAZOL	ChEMBL	Phase 4 (approved)	ESR1
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	ESR1
DEQUALINIUM	ChEMBL	Phase 4 (approved)	ESR1
DESOGESTREL	ChEMBL	Phase 4 (approved)	ESR1
DIENESTROL	ChEMBL	Phase 4 (approved)	ESR1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	ESR1
DINOPROSTONE	ChEMBL	Phase 4 (approved)	ESR1
DOXORUBICIN	ChEMBL	Phase 4 (approved)	ESR1
DRONEDARONE	ChEMBL	Phase 4 (approved)	ESR1
ELACESTRANT	ChEMBL	Phase 4 (approved)	ESR1
ERGOCALCIFEROL	ChEMBL	Phase 4 (approved)	ESR1
ERTAPENEM	ChEMBL	Phase 4 (approved)	ESR1
ESTETROL	ChEMBL	Phase 4 (approved)	ESR1
ESTRADIOL	ChEMBL	Phase 4 (approved)	ESR1
ESTRADIOL CYPIONATE	ChEMBL	Phase 4 (approved)	ESR1
ESTRADIOL VALERATE	ChEMBL	Phase 4 (approved)	ESR1
ESTRAMUSTINE	ChEMBL	Phase 4 (approved)	ESR1
ESTRIOL	ChEMBL	Phase 4 (approved)	ESR1
ESTRONE	ChEMBL	Phase 4 (approved)	ESR1
ETHINYL ESTRADIOL	ChEMBL	Phase 4 (approved)	ESR1
ETHYLESTRENOL	ChEMBL	Phase 4 (approved)	ESR1
ETHYNODIOL DIACETATE	ChEMBL	Phase 4 (approved)	ESR1
ETONOGESTREL	ChEMBL	Phase 4 (approved)	ESR1
ETRAVIRINE	ChEMBL	Phase 4 (approved)	ESR1
FLUPIRTINE	ChEMBL	Phase 4 (approved)	ESR1
HEXACHLOROPHENE	ChEMBL	Phase 4 (approved)	ESR1
HEXESTROL	ChEMBL	Phase 4 (approved)	ESR1
IBUPROFEN	ChEMBL	Phase 4 (approved)	ESR1
ISOCONAZOLE	ChEMBL	Phase 4 (approved)	ESR1
LASOFOXIFENE	ChEMBL	Phase 4 (approved)	ESR1
LENVATINIB	ChEMBL	Phase 4 (approved)	ESR1
LEVONORGESTREL	ChEMBL	Phase 4 (approved)	ESR1
LUSUTROMBOPAG	ChEMBL	Phase 4 (approved)	ESR1
LYMECYCLINE	ChEMBL	Phase 4 (approved)	ESR1