> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/zanzalintinib-0a1dc103-7c01-43a8-bc9a-bbc2b2e81de6
> Record changed: 2026-10-13

# Zanzalintinib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

**Drug name**

Zanzalintinib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

**Molecular weight**

528.54

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

**Structure (SMILES)**

CNC(=O)c1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)ccnc2cc1OC

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

### Other names (13)

- xl 092
- Xl 092
- XL-092
- xl092
- XL092
- zanzalintinib
- Zanzalintinib
- zanzalintinib \[INN\]
- ZANZALINTINIB \[USAN\]
- Zanzalintinib \[WHO-DD\]
- zanzalintinib inn
- zanzalintinib usan
- zanzalintinib who dd

## Identifiers

**CAS registry numbers**

- 2367004-54-2

**ChEMBL ID**

CHEMBL5314428

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

**InChIKey**

JSPCKALGNNVYOO-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5314428)

**PubChem compound IDs**

- 139350422

**FDA ingredient codes (UNII)**

- KC2JC2ZA04

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

zanzalintinib

**Type**

Synthetic organic

**Drug name stem**

\-tinib

### Mechanisms of action (3)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
MET proto-oncogene, receptor tyrosine kinase

**Gene symbol**  
MET

**Protein identifier**  
P08581

**Median affinity**  
8

**Affinity units**  
pIC50
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
AXL receptor tyrosine kinase

**Gene symbol**  
AXL

**Protein identifier**  
P30530

**Median affinity**  
8

**Affinity units**  
pIC50
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
MER proto-oncogene, tyrosine kinase

**Gene symbol**  
MERTK

**Protein identifier**  
Q12866

**Median affinity**  
8

**Affinity units**  
pIC50

### Investigated indications (7)

- **Condition**  
Carcinoma, Squamous Cell

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000181

**Subject identifier**  
D002294
- **Condition**  
Carcinoma, Renal Cell

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000349

**Subject identifier**  
D002292
- **Condition**  
Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Carcinoma, Renal Cell

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000681

**Subject identifier**  
D002292
- **Condition**  
Carcinoma, Non-Small-Cell Lung

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0003060

**Subject identifier**  
D002289
- **Condition**  
Carcinoma, Renal Cell

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0005708

**Subject identifier**  
D002292
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0005575

**Subject identifier**  
D015179

### Open Targets indications (37)

- **Condition identifier**  
EFO\_0000181
- **Condition identifier**  
EFO\_0000349

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0000681

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0005708

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_1001480

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0002142

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0002715

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0004958

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005005

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005040

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005058

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005060

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005070
- **Condition identifier**  
MONDO\_0005086

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005102

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005549

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005575

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0006329

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0006382

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0006468

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0007256

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008315

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008977

**Highest recorded phase**  
2

And 12 more, listed on the interactive page.

### Trial references (5)

- NCT03337698  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03337698)
- NCT05425940  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05425940)
- NCT05678673  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05678673)
- NCT06082167  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06082167)
- NCT06191796  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06191796)

## Chemical properties

**Hydrogen bond acceptors**

6

**Hydrogen bond donors**

3

**Polar surface area**

118.65

**Calculated partition coefficient (ALogP)**

4.89

**Calculated partition coefficient (XLogP)**

4.7

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

1

**Rotatable bonds**

8

**Heavy atoms**

39

**Molecular formula**

C29H25FN4O5

**Monoisotopic mass**

528.18089807

**Natural product**

No

## Evidence counts

**Recorded assays**

116

**Active assays**

10

### Active assay types

- Confirmatory

## Related records

### Trials (49)

- A Clinical Study of Belzutifan (MK-6482) and Zanzalintinib in People With Renal Cell Carcinoma (RCC) (LITESPARK-034/LS-034/MK-6482-034)
- A Clinical Study of Belzutifan and Zanzalintinib in People With Recurrent Kidney Cancer Following Adjuvant Therapy (MK-6482-033)
- A Phase 2 Multicenter Single-Arm Clinical Trial of Zanzalintinib and Pembrolizumab in Subjects With Resectable Clear Cell Renal Cell Carcinoma
- A Phase 2 Study Of Zanzalintinib For Patients With Recurrent Or Metastatic Olfactory Neuroblastoma
- A Phase 2 Trial of Zanzalintinib in Advanced/Metastatic Bone Sarcomas (ZAMBONE)
- A Study Of Multiple Immunotherapy-Based Treatment Combinations In Participants With Metastatic Non-Small Cell Lung Cancer (Morpheus- Non-Small Cell Lung Cancer)
- [A Study of XB628 Alone and in Combination With Zanzalintinib in Participants With Recurrent Advanced or Metastatic Solid Tumors](https://trialight.com/data/trial/a-study-of-xb628-alone-and-in-combination-with-zanzalintinib-7e263e48-4a8e-4cf2-8d3f-a0ee66365f68.md)
- A Study of XL092 as Single-Agent and Combination Therapy in Subjects With Solid Tumors
- A Study of Zanzalintinib in Participants With Recurrent or Progressive Meningioma
- Dose Finding Study of Zanzalintinib With Pembrolizumab and Cetuximab in Head and Neck SCC
- H&N NEO-COMBAT XL: Neoadjuvant XL-092 (Zanzalintinib) and Pembrolizumab (Keytruda) in Surgically Resectable, HPV Negative Oral Cavity Squamous Cell Carcinoma (OCSCC)
- [Long-Term Extension Study for Participants Previously Enrolled in an Exelixis-Sponsored Study](https://trialight.com/data/trial/long-term-extension-study-for-participants-previously-1f9d623b-4584-41d7-bd30-d9e8f8906175.md)
- Maintenance Zanzalintinib and Durvalumab in Participants With Advanced Hepatocellular Cancer
- Maintenance Zanzalintinib With Etoposide After HDCT in GCT
- Neoadjuvant Zanzalintinib Plus Nivolumab in Patients With Locally Advanced and/or Inoperable Clear Cell Renal Cell Carcinoma With or Without Non-measurable Metastasis
- NIMBLE-CRC: NeoImmunoModulation Before Leveraging Excision in Colorectal Rectal Cancer
- Pharmacokinetics (PK) and Safety of Zanzalintinib in Participants With Moderate Hepatic Impairment (HI)
- Phase 2 Trial of Zanzalintinib and Pembrolizumab in Select Subtypes of Advanced/Metastatic Soft-tissue Sarcoma
- Phase II Trial of Zanzalitinib in Patients With Metastatic Castration Resistant Prostate Cancer
- Study of XL092 + Atezolizumab vs Regorafenib in Participants With Metastatic Colorectal Cancer

### In development for (8)

- Bone sarcoma Phase 2
- [Clear cell renal carcinoma](https://trialight.com/data/condition/clear-cell-renal-carcinoma-789eee25-ec64-5771-9b7d-d19544781b11.md) Phase 3
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 3
- [Head and neck squamous cell carcinoma](https://trialight.com/data/condition/head-and-neck-squamous-cell-carcinoma-cbc3ae58-4a6c-52e4-a41b-274051db19fa.md) Phase 2
- Neoplasm Phase 2
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 1
- Renal cell adenocarcinoma Phase 3
- [Renal cell carcinoma](https://trialight.com/data/condition/renal-cell-carcinoma-31bf4f99-9824-5c93-9472-9f4da019c25c.md) Phase 3

---

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