Mobocertinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Mobocertinib is an ofm drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2021. Its mechanism of action is classified as Cytochrome P450 3A Inducers and HER1 Antagonists. DrugCentral lists 7 molecular targets, including ERBB4, BLK and ERBB2. Recorded indications include Advanced or metastatic non-small cell lung cancer with EGFR exon 20 insertion mutations.

• Approval status: ofm (first approved 2021 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Cytochrome P450 3A Inducers; HER1 Antagonists.
• Molecular targets: ERBB4, BLK, ERBB2 and JAK3 (7 listed in DrugCentral).
• Indications: Advanced or metastatic non-small cell lung cancer with EGFR exon 20 insertion mutations.
• ATC code: L01EB10 (Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors).
• Molecular formula: C32H39N7O4; molecular weight 585.71 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Advanced or metastatic non-small cell lung cancer with EGFR exon 20 insertion mutations

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 3A Inducers; HER1 Antagonists
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (7)

Target	Gene	Action	Activity
Receptor tyrosine-protein kinase erbB-4	ERBB4	inhibitor	IC50 10.00
Tyrosine-protein kinase Blk	BLK	inhibitor	IC50 9.70
Receptor tyrosine-protein kinase erbB-2	ERBB2	inhibitor	IC50 9.40
Tyrosine-protein kinase JAK3	JAK3	inhibitor	IC50 8.66
Tyrosine-protein kinase TXK	TXK	inhibitor	IC50 8.64
Tyrosine-protein kinase BTK	BTK	inhibitor	IC50 8.55
Epidermal growth factor receptor	EGFR	inhibitor	Kd 6.67

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2021-09-15	FDA	—	TAKEDA PHARMS USA	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EB10	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label
• FDA label: EGFR · Testing Required
• HCSC label

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Diarrhoea	235.9
Metastases to central nervous system	85.2
Death	68.5
Dry skin	61.2
Rash	56.0
Non-small cell lung cancer	52.6
Malignant neoplasm progression	52.3
Decreased appetite	47.2

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Mobocertinib is on its molecule page.

• Molecular formula: C₃₂H₃₉N₇O₄
• Molecular weight: 585.71 g/mol
• CAS number: 1847461-43-1
• InChIKey: AZSRSNUQCUDCGG-UHFFFAOYSA-N
• PubChem CID: 118607832

CC(C)OC(=O)C1=CN=C(N=C1C2=CN(C3=CC=CC=C32)C)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Mobocertinib used for?

DrugCentral lists the following indications for Mobocertinib: Advanced or metastatic non-small cell lung cancer with EGFR exon 20 insertion mutations.

How does Mobocertinib work?

Mobocertinib is classified as Cytochrome P450 3A Inducers and HER1 Antagonists; its molecular targets in DrugCentral include ERBB4 (inhibitor), BLK (inhibitor), ERBB2 (inhibitor) and JAK3 (inhibitor).

When was Mobocertinib first approved?

Mobocertinib was first approved by the FDA in 2021.

What drug class does Mobocertinib belong to?

Mobocertinib is in the Kinase Inhibitor class.

What is the chemical formula of Mobocertinib?

Mobocertinib has the molecular formula C32H39N7O4 and a molecular weight of 585.71 g/mol.

Sources

• DrugCentral drug card 5471 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL4650319 — compound record and bioactivity
• PubChem CID 118607832 — chemical identifiers
• DrugBank DB16390 — drug record
• FDA UNII 39HBQ4A67L — substance identity
• DailyMed: FDA labels for Mobocertinib — current prescribing information (label search)
• UniProt Q15303 (ERBB4) — target protein
• UniProt P51451 (BLK) — target protein
• UniProt P04626 (ERBB2) — target protein
• UniProt P52333 (JAK3) — target protein
• UniProt P42681 (TXK) — target protein
• UniProt Q06187 (BTK) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.