Sunvozertinib

Summary

Sunvozertinib (CHEMBL5314564) is a phase-3 clinical-stage small molecule targeting EGFR and BTK; indicated across 3 conditions including non-small cell lung carcinoma and neoplasm of mature b-cells; with CIViC clinical evidence for 7 variant-indication associations (e.g. EGFR D770_N771insGT OR EGFR D770_N771insD OR EGFR D770_N771insF OR EGFR D770_N771insGD OR EGFR D770_N771insT OR EGFR N771delinsCH OR EGFR N771delinsGF OR EGFR N771delinsRD OR EGFR N771delinsSQRGH OR EGFR N771_P772insDN in lung non-small cell carcinoma).

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 2 (EGFR, BTK)
• Indications: 3 conditions
• Clinical trials: 19
• Precision-oncology evidence (CIViC): 7 variant–indication associations
• Chemistry: 584.1 Da · C29H35ClFN7O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5314564
Name	Sunvozertinib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	139377809
Molecular formula	C29H35ClFN7O3
Molecular weight	584.1
InChIKey	BTMKEDDEMKKSEF-QGZVFWFLSA-N

SMILES: CC(C)(C1=CC(=C(C=C1NC2=NC(=NC=C2)NC3=C(C=C(C(=C3)NC(=O)C=C)N4CC[C@H](C4)N(C)C)OC)Cl)F)O

IUPAC name: N-[5-[[4-[5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)anilino]pyrimidin-2-yl]amino]-2-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-4-methoxyphenyl]prop-2-enamide

Also known as: A-1801, A1801, ASYM-122507, DZ'0586, DZ-0586, DZ00000586, DZ0586, DZD-9008, Dzd9008, DZD9008, Sunvozertinib, SUNVOZERTINIB

Patent coverage: 8 distinct patent families (24 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 16 (67%) 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
EGFR	epidermal growth factor receptor	Inhibition	7.09	17.5%	P00533
BTK	Bruton tyrosine kinase	Inhibition	8.54	0.7%	Q06187

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Epidermal growth factor receptor.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
EGFR	7.7	IC50	19.95	nM	CHEMBL_ACT_29225447
EGFR	7.6	IC50	25.12	nM	CHEMBL_ACT_29225396
EGFR	7.5	IC50	31.62	nM	CHEMBL_ACT_29225379
EGFR	7.3	IC50	50.12	nM	CHEMBL_ACT_29224925

Target pathways

Aggregated over 2 target gene(s): EGFR, BTK.

Top Reactome pathways

82 total, by targets touching each:

Pathway	Targets	Genes
Signaling by ERBB2	1	EGFR
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants	1	EGFR
Signaling by ERBB4	1	EGFR
ER-Phagosome pathway	1	BTK
Antigen processing-Cross presentation	1	BTK
SHC1 events in ERBB2 signaling	1	EGFR
PLCG1 events in ERBB2 signaling	1	EGFR
PIP3 activates AKT signaling	1	EGFR
Adaptive Immune System	1	BTK
Signal Transduction	1	BTK
Disease	1	BTK
Toll Like Receptor 4 (TLR4) Cascade	1	BTK
MyD88:MAL(TIRAP) cascade initiated on plasma membrane	1	BTK
Toll Like Receptor TLR1:TLR2 Cascade	1	BTK
Toll Like Receptor TLR6:TLR2 Cascade	1	BTK
Innate Immune System	1	BTK
Immune System	1	BTK
Toll-like Receptor Cascades	1	BTK
Signaling by EGFR	1	EGFR
GRB2 events in EGFR signaling	1	EGFR
GAB1 signalosome	1	EGFR
SHC1 events in EGFR signaling	1	EGFR
Toll Like Receptor 2 (TLR2) Cascade	1	BTK
EGFR downregulation	1	EGFR
Signaling by Rho GTPases	1	BTK
RHO GTPase Effectors	1	BTK
GRB2 events in ERBB2 signaling	1	EGFR
PI3K events in ERBB2 signaling	1	EGFR
Fcgamma receptor (FCGR) dependent phagocytosis	1	BTK
Regulation of actin dynamics for phagocytic cup formation	1	BTK

Dominant GO biological processes

GO term	Targets
protein phosphorylation	2
cell morphogenesis	1
ossification	1
embryonic placenta development	1
positive regulation of protein phosphorylation	1
hair follicle development	1
ubiquitin-dependent protein catabolic process	1
signal transduction	1
cell surface receptor signaling pathway	1
epidermal growth factor receptor signaling pathway	1
salivary gland morphogenesis	1
learning or memory	1
positive regulation of cell population proliferation	1
gene expression	1
protein ubiquitination	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
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
neoplasm of mature B-cells	1	MONDO:0004949	EFO:0000096
liver disorder	1	MONDO:0005154	EFO:0001421

Clinical trials

Total trials: 19.

Phase distribution

Phase	Trials
PHASE2	6
PHASE1	5
PHASE1/PHASE2	4
PHASE3	2
Not specified	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05668988	PHASE3	ACTIVE_NOT_RECRUITING	A Study of DZD9008 Versus Platinum-Based Doublet Chemotherapy in Local Advanced or Metastatic Non-small Cell Lung Cancer (WU-KONG28)
NCT07182682	PHASE3	RECRUITING	A Phase 3 Study of Sunvozertinib Versus Placebo as Adjuvant Therapy in Patients With Early-Stage Non-Small Cell Lung Cancer Harboring EGFR Exon 20 Insertion Mutations or PACC Mutations After Radical Surgery
NCT03974022	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Assessing an Oral EGFR Inhibitor, Sunvozertinib in Patients Who Have Advanced Non-small Cell Lung Cancer With EGFR or HER2 Mutation (WU-KONG1)
NCT05712902	PHASE2	ACTIVE_NOT_RECRUITING	Sunvozertinib (DZD9008) in Pretreated Lung Cancer Patients with EGFR Exon20 Insertion Mutation (WU-KONG6)
NCT06195189	PHASE1/PHASE2	RECRUITING	Sunvozertinib Combined With Chemotherapy for EGFRm After EGFR-TKI Treatment Failure：Phase I/II
NCT06295432	PHASE2	RECRUITING	A Phase II Clinical Trial of DZD9008 in Combination With AZD4205 in Standard Treatment Failed NSCLC Patients With EGFR Mutations (WU-KONG21)
NCT06563999	PHASE2	RECRUITING	Neoadjuvant Umbrella Trial for Patients With Unresectable Stage III NSCLC Harboring Rare Mutations.
NCT06864624	PHASE2	RECRUITING	Perioperative Treatment of Sunvozertinib in Stage II-IIIB NSCLC
NCT07079475	PHASE1/PHASE2	RECRUITING	Study of Oral EGFR Inhibitor DZD6008 Combined With Sunvozertinib in Patients Who Have Advanced NSCLC With EGFR Mutations (TIAN-SHAN8)
NCT07117890	PHASE2	RECRUITING	Sunvozertinib Treatment in Untreated Advanced NSCLC With EGFR Uncommon Mutations
NCT07274761	PHASE2	ACTIVE_NOT_RECRUITING	Neoadjuvant Sunvozertinib in Stage II-IIIB Non-small Cell Lung Cancer Harboring EGFR Exon 20 Insertion Mutation.
NCT04148742	PHASE1/PHASE2	WITHDRAWN	Assessing an Oral Bruton Tyrosine Kinase Inhibitor, DZD9008 in Patients Who Have Non-Hodgkin B-cell Lymphoma (WU-KONG3)
NCT06905197	PHASE1	RECRUITING	A Multinational Study Assessing an Oral EGFR Inhibitor, DZD6008 in Patients Who Have Advanced NSCLC With EGFR Mutations (TIAN-SHAN1)
NCT04909242	PHASE1	COMPLETED	Assessing the Safety, Tolerability and Pharmacokinetics(PK) of DZD9008 and the Effect of Low-fat Meal on PK of DZD9008 in Healthy Adult Participants
NCT05418582	PHASE1	COMPLETED	Drug-drug Interactions Between DZD9008 and Itraconazole/Carbamazepine
NCT05926180	PHASE1	COMPLETED	Assessing the Effect of DZD9008 on the Pharmacokinetics of the Cocktail Probes Representative for CYP3A4, P-gp, BCRP and OATP1B1 in Patients with EGFR or HER2 Mutant Advanced Non-small Cell Lung Cancer (WU-KONG19)
NCT06084104	PHASE1	COMPLETED	DZD9008 PK Study in Hepatic Impairment Subjects
NCT05559645	Not specified	RECRUITING	Assessing an Oral EGFR Inhibitor, DZD9008 in Patients With Advanced Non-small Cell Lung Cancer(NSCLC) With EGFR Mutations (WU-KONG15)
NCT06786208	Not specified	NOT_YET_RECRUITING	Real-world Study of Sunvozertinib Treatment in Advanced EGFR-Mutant NSCLC After EGFR-TKI Treatment Failure

Clinical evidence (CIViC)

Variant × indication × effect (7 predictive associations from 7 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
EGFR D770_N771insGT OR EGFR D770_N771insD OR EGFR D770_N771insF OR EGFR D770_N771insGD OR EGFR D770_N771insT OR EGFR N771delinsCH OR EGFR N771delinsGF OR EGFR N771delinsRD OR EGFR N771delinsSQRGH OR EGFR N771_P772insDN	Lung Non-small Cell Carcinoma	Sensitivity/Response	Sunvozertinib	CIViC A	EID12632
EGFR D770delinsGY OR EGFR D770_N771insY OR EGFR N771_P772insT OR EGFR H773_V774insGNPH OR EGFR A767_S768insTLA OR EGFR S768_V769insLDS OR EGFR V769_D770insCV OR EGFR V769_D770insGA OR EGFR V769_D770insGVASV OR EGFR D770delinsAS	Lung Non-small Cell Carcinoma	Sensitivity/Response	Sunvozertinib	CIViC A	EID12631
EGFR Exon 20 Insertion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Sunvozertinib	CIViC A	EID12718
EGFR H773_V774insH OR EGFR D770_N771insG OR EGFR H773_V774insNPH OR EGFR A763_Y764insFQEA OR EGFR V774_C775insHV OR EGFR H773_V774insPH OR EGFR H773_V774insAH OR EGFR D770_N771insH OR EGFR N771dup	Lung Non-small Cell Carcinoma	Sensitivity/Response	Sunvozertinib	CIViC A	EID12630
EGFR H773delinsYNPY OR EGFR H773delinsYPNPY OR EGFR H773_V774insHPH OR EGFR H773_V774insTH OR EGFR C775_R776insNPHVC	Lung Non-small Cell Carcinoma	Sensitivity/Response	Sunvozertinib	CIViC A	EID12634
EGFR N771delinsGY OR EGFR P772_H773insYNP OR EGFR N771_P772insRH OR EGFR N771_P772insVDN OR EGFR P772delinsHR OR EGFR P772_H773insDNP OR EGFR P772_H773insPHP OR EGFR P772_H773insQ OR EGFR P772_H773insRNP OR EGFR H773delinsNPY OR EGFR H773delinsPNPY	Lung Non-small Cell Carcinoma	Sensitivity/Response	Sunvozertinib	CIViC A	EID12633
EGFR S768_D770dup OR EGFR A767_V769dupASV	Lung Non-small Cell Carcinoma	Sensitivity/Response	Sunvozertinib	CIViC A	EID12623

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

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

Molecule	Source	Status	Shared targets
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR
DACOMITINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR
MOBOCERTINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR
SELUMETINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR
ACALABRUTINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
BOSUTINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
BRIGATINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
CERITINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
DASATINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
FEDRATINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
IBRUTINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
MITOXANTRONE	ChEMBL	Phase 4 (approved)	BTK, EGFR
NERATINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
OLMUTINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
OSIMERTINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
PONATINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
SUNITINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
VANDETANIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
ZANUBRUTINIB	ChEMBL	Phase 4 (approved)	BTK, EGFR
ABIVERTINIB	ChEMBL	Phase 3	BTK, EGFR
ALISERTIB	ChEMBL	Phase 3	BTK, EGFR
CANERTINIB	ChEMBL	Phase 3	BTK, EGFR
CEDIRANIB	ChEMBL	Phase 3	BTK, EGFR
DOVITINIB	ChEMBL	Phase 3	BTK, EGFR
EVOBRUTINIB	ChEMBL	Phase 3	BTK, EGFR
LESTAURTINIB	ChEMBL	Phase 3	BTK, EGFR
ORELABRUTINIB	ChEMBL	Phase 3	BTK, EGFR
POZIOTINIB	ChEMBL	Phase 3	BTK, EGFR
PYROTINIB	ChEMBL	Phase 3	BTK, EGFR
REMIBRUTINIB	ChEMBL	Phase 3	BTK, EGFR
ROCILETINIB	ChEMBL	Phase 3	BTK, EGFR
SARACATINIB	ChEMBL	Phase 3	BTK, EGFR
TESEVATINIB	ChEMBL	Phase 3	BTK, EGFR
TOLEBRUTINIB	ChEMBL	Phase 3	BTK, EGFR
APITOLISIB	ChEMBL	Phase 2	BTK, EGFR
ATUZABRUTINIB	ChEMBL	Phase 2	BTK, EGFR
BRANEBRUTINIB	ChEMBL	Phase 2	BTK, EGFR
CENISERTIB	ChEMBL	Phase 2	BTK, EGFR
DEFOSBARASERTIB	ChEMBL	Phase 2	BTK, EGFR
FORETINIB	ChEMBL	Phase 2	BTK, EGFR
ILORASERTIB	ChEMBL	Phase 2	BTK, EGFR
PELITINIB	ChEMBL	Phase 2	BTK, EGFR
R-406	ChEMBL	Phase 2	BTK, EGFR
SPEBRUTINIB	ChEMBL	Phase 2	BTK, EGFR
SU-014813	ChEMBL	Phase 2	BTK, EGFR
TOZASERTIB	ChEMBL	Phase 2	BTK, EGFR
Binimetinib	PubChem	Approved	BTK, EGFR
Pazopanib	PubChem	Approved	BTK, EGFR
RITLECITINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK
ABEMACICLIB	ChEMBL	Phase 4 (approved)	EGFR
AFATINIB DIMALEATE	ChEMBL	Phase 4 (approved)	EGFR
ALECTINIB	ChEMBL	Phase 4 (approved)	EGFR
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	EGFR
AXITINIB	ChEMBL	Phase 4 (approved)	EGFR
BACITRACIN	ChEMBL	Phase 4 (approved)	EGFR
BITHIONOL	ChEMBL	Phase 4 (approved)	EGFR
CABOZANTINIB	ChEMBL	Phase 4 (approved)	EGFR
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	EGFR
CHROMIC CHLORIDE	ChEMBL	Phase 4 (approved)	EGFR