All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

mobocertinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5471	1847461-43-1

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: mobocertinib mobocertinib succinate exkivity TAK-788 AP32788

Mobocertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR) that irreversibly binds to and inhibits EGFR exon 20 insertion mutations at lower concentrations than wild type (WT) EGFR. Two pharmacologically-active metabolites (AP32960 and AP32914) with similar inhibitory profiles to mobocertinib have been identified in the plasma after oral administration of mobocertinib. In vitro, mobocertinib also inhibited the activity of other EGFR family members (HER2 and HER4) and one additional kinase (BLK) at clinically relevant concentrations (IC50 values <2 nM). Molecular weight: 585.71 Formula: C32H39N7O4 CLOGP: 5.48 LIPINSKI: 3 HAC: 11 HDO: 2 TPSA: 113.85 ALOGS: -4.63 ROTB: 13 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Sept. 15, 2021	FDA	TAKEDA PHARMS USA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Diarrhoea	135.16	42.80	88	627	715278	62773029

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Diarrhoea	69.27	54.04	37	180	389875	34566839

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Diarrhoea	153.61	43.38	100	728	880389	78863171
Metastases to central nervous system	43.65	43.38	13	815	16362	79727198

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EB10	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
FDA MoA	N0000020010	HER1 Antagonists
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000190118	Cytochrome P450 3A Inducers

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Advanced or metastatic non-small cell lung cancer with EGFR exon 20 insertion mutations	indication	703228009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 40MG BASE	EXKIVITY	TAKEDA PHARMS USA	N215310	Sept. 15, 2021	RX	CAPSULE	ORAL	10227342	May 13, 2035	TREATMENT OF PATIENTS WITH NON-SMALL CELL LUNG CANCER (NSCLC) WITH EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 20 EXON INSERTION MUTATIONS WHOSE DISEASE HAS PROGRESSED ON OR AFTER PLATINUM-BASED CHEMOTHERAPY

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 40MG BASE	EXKIVITY	TAKEDA PHARMS USA	N215310	Sept. 15, 2021	RX	CAPSULE	ORAL	Sept. 15, 2026	NEW CHEMICAL ENTITY
EQ 40MG BASE	EXKIVITY	TAKEDA PHARMS USA	N215310	Sept. 15, 2021	RX	CAPSULE	ORAL	Sept. 15, 2028	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) EXON 20 INSERTION MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, WHOSE DISEASE HAS PROGRESSED ON OR AFTER PLATINUM-BASED CHEMOTHERAPY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN	INHIBITOR	Kd	6.67		DRUG LABEL	DRUG LABEL
Receptor tyrosine-protein kinase erbB-2	Kinase	P04626	ERBB2_HUMAN	INHIBITOR	IC50	9.40		DRUG LABEL	DRUG LABEL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN	INHIBITOR	IC50	8.55		DRUG LABEL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN	INHIBITOR	IC50	8.66		DRUG LABEL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN	INHIBITOR	IC50	9.70		DRUG LABEL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN	INHIBITOR	IC50	8.64		DRUG LABEL
Receptor tyrosine-protein kinase erbB-4	Kinase	Q15303	ERBB4_HUMAN	INHIBITOR	IC50	10		DRUG LABEL

External reference:

ID	Source
39HBQ4A67L	UNII
2389149-74-8	SECONDARY_CAS_RN
C5418176	UMLSCUI
CHEMBL4650319	ChEMBL_ID
118607832	PUBCHEM_CID
DB16390	DRUGBANK_ID
D12001	KEGG_DRUG
CHEMBL4802239	ChEMBL_ID
11183	INN_ID
10468	IUPHAR_LIGAND_ID
018847	NDDF
018848	NDDF
4040829	VANDF
2570736	RXNORM
350405	MMSL
39900	MMSL
d09808	MMSL
C000720862	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
EXKIVITY	HUMAN PRESCRIPTION DRUG LABEL	1	63020-040	CAPSULE	40 mg	ORAL	NDA	33 sections
EXKIVITY	HUMAN PRESCRIPTION DRUG LABEL	1	63020-040	CAPSULE	40 mg	ORAL	NDA	33 sections
EXKIVITY	HUMAN PRESCRIPTION DRUG LABEL	1	63020-040	CAPSULE	40 mg	ORAL	NDA	33 sections