Sitagliptin - PharmaKB

Januvia(sitagliptin)

Brynovin, Efficib, Janumet, Januvia, Juvisync, Ristaben, Ristfor, Sitagliptin, Sitagliptin / Metformin, Steglujan, Tesavel, Velmetia, Xelevia, Zituvimet, Zituvio (sitagliptin) is a small molecule pharmaceutical. Sitagliptin was first approved as Januvia on 2006-10-16. It is used to treat type 2 diabetes mellitus in the USA. It has been approved in Europe to treat type 2 diabetes mellitus. The pharmaceutical is active against dipeptidyl peptidase 4.

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Commercial

Clinical

Drug

Target

Variants

Financial

Trends

Safety

Events Timeline

YTD

Max

Events

FDA approval date

EMA approval date

Patent expiration date

Study first post date

Last update post date

Start date

Primary completion date

Completion date

Results first post date

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Commercial

Therapeutic Areas

Therapeutic Area	MeSH
nutritional and metabolic diseases	D009750
endocrine system diseases	D004700

Trade Name

FDA

EMA

Brynovin, Januvia, Zituvio

Combinations

Janumet, Steglujan, Zituvimet (discontinued: Juvisync)

Drug Products

FDA

EMA

New Drug Application (NDA)

Abbreviated New Drug Application (ANDA)

Metformin hydrochloride

Sitagliptin phosphate

Tradename	Company	Number	Date	Products
JANUMET	Merck & Co	N-022044 RX	2007-03-30	2 products, RLD, RS
JANUMET XR	Merck & Co	N-202270 RX	2012-02-02	3 products, RLD, RS

Sitagliptin phosphate

Tradename	Company	Number	Date	Products
JANUVIA	Merck & Co	N-021995 RX	2006-10-16	3 products, RLD, RS

Simvastatin

Sitagliptin phosphate

Tradename	Company	Number	Date	Products
JUVISYNC	Merck & Co	N-202343 DISCN	2011-10-07	6 products, RLD

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Ertugliflozin

Sitagliptin phosphate

Tradename	Company	Number	Date	Products
STEGLUJAN	Merck & Co	N-209805 RX	2017-12-19	2 products, RLD, RS

Sitagliptin

Tradename	Company	Number	Date	Products
ZITUVIO	Zydus Therapeutics	N-211566 RX	2023-10-18	3 products, RLD, RS

Metformin hydrochloride

Sitagliptin

Tradename	Company	Number	Date	Products
ZITUVIMET	Zydus Therapeutics	N-216743 RX	2023-11-03	2 products, RLD, RS
ZITUVIMET XR	Zydus Therapeutics	N-216778 RX	2024-07-18	3 products, RLD, RS

Sitagliptin hydrochloride

Tradename	Company	Number	Date	Products
BRYNOVIN	Azurity	N-219122 RX	2025-01-16	1 products, RLD, RS

Labels

FDA

EMA

Brand Name	Status	Last Update
janumet	New Drug Application	2025-03-25
januvia	New Drug Application	2024-11-14
sitagliptin	NDA authorized generic	2025-01-31
sitagliptin - metformin	Export only	2023-04-14
sitagliptin and metformin hydrochloride	NDA authorized generic	2024-08-31
steglujan	New Drug Application	2024-12-20
zituvimet	New Drug Application	2024-08-09
zituvimet xr	New Drug Application	2024-07-23
zituvio	New Drug Application	2025-01-31

Indications

FDA

EMA

Indication	Ontology	MeSH	ICD-10
type 2 diabetes mellitus	EFO_0001360	D003924	E11
hypercholesterolemia	—	D006937	—
coronary artery disease	—	D003324	I25.1
hypertriglyceridemia	EFO_0004211	D015228	—
hyperlipoproteinemias	—	D006951	—

Agency Specific

FDA

EMA

Expiration	Code
ERTUGLIFLOZIN / SITAGLIPTIN PHOSPHATE, STEGLUJAN, MSD SUB MERCK
2024-09-17	M-275
METFORMIN HYDROCHLORIDE / SITAGLIPTIN PHOSPHATE, JANUMET, MSD SUB MERCK
2024-06-04	PED
2023-12-04	M-187
2023-02-12	PED
METFORMIN HYDROCHLORIDE / SITAGLIPTIN PHOSPHATE, JANUMET XR, MERCK SHARP DOHME
2024-06-04	PED
2023-12-04	M-187
2023-02-12	PED
SITAGLIPTIN PHOSPHATE, JANUVIA, MERCK SHARP DOHME
2024-06-04	PED
2023-12-04	M-187
2023-02-12	PED

Patent Expiration

Patent	Expires	Flag	FDA Information
Ertugliflozin / Sitagliptin Phosphate, Steglujan, Msd Sub Merck
9308204	2030-10-21	DP
9439901	2030-10-21		U-2214
8080580	2030-07-13	DS, DP	U-2214
7326708	2026-11-24	DS, DP	U-802, U-1188, U-1227, U-2214
Metformin Hydrochloride / Sitagliptin Phosphate, Janumet, Msd Sub Merck
8414921	2028-07-21	DP	U-1036

ATC Codes

A: Alimentary tract and metabolism drugs

— A10: Drugs used in diabetes

— A10B: Blood glucose lowering drugs, excl. insulins

— A10BD: Combinations of oral blood glucose lowering drugs

— A10BD07: Metformin and sitagliptin

— A10BD12: Pioglitazone and sitagliptin

— A10BD24: Sitagliptin and ertugliflozin

— A10BH: Dipeptidyl peptidase 4 (dpp-4) inhibitors for blood glucose lowering

— A10BH01: Sitagliptin

— A10BH51: Sitagliptin and simvastatin

HCPCS

No data

Clinical

Clinical Trials

537 clinical trials

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Indications Phases 4

Indication	MeSH	Ontology	ICD-10	Ph 1	Ph 2	Ph 3	Ph 4	Other	Total
Type 2 diabetes mellitus	D003924	EFO_0001360	E11	45	37	133	98	78	387
Diabetes mellitus	D003920	EFO_0000400	E08-E13	22	38	128	83	49	313
Healthy volunteers/patients	—	—	—	16	—	1	3	2	22
Type 1 diabetes mellitus	D003922	EFO_0001359	E10	3	7	2	7	3	19
Heart failure	D006333	EFO_0003144	I50	1	—	—	5	5	11
Obesity	D009765	EFO_0001073	E66.9	2	1	—	4	3	10
Non-alcoholic fatty liver disease	D065626	EFO_0003095	K75.81	—	2	—	4	3	9
Fatty liver	D005234	EFO_0003934	—	—	2	—	4	3	9
Hyperglycemia	D006943	—	R73.9	—	—	—	7	2	9
Cardiovascular diseases	D002318	EFO_0000319	I98	—	—	2	2	4	8

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Indications Phases 3

Indication	MeSH	Ontology	ICD-10	Ph 1	Ph 2	Ph 3	Ph 4	Other	Total
Renal insufficiency	D051437	—	N19	1	—	6	—	—	7
Fibrosis	D005355	—	—	1	1	1	—	2	5
Inflammation	D007249	MP_0001845	—	—	2	1	—	1	4
Cystic fibrosis	D003550	EFO_0000390	E84	1	1	1	—	1	4
Hyperlipidemias	D006949	EFO_0003774	E78.5	—	1	3	—	—	3
Graft vs host disease	D006086	—	D89.81	—	2	1	—	—	3
Chronic renal insufficiency	D051436	—	N18	—	—	2	—	1	3
Kidney diseases	D007674	EFO_0003086	N08	—	—	2	—	1	3
Inferior wall myocardial infarction	D056989	EFO_1000983	—	—	1	2	—	—	2
Covid-19	D000086382	—	U07.1	—	—	1	—	1	2

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Indications Phases 2

Indication	MeSH	Ontology	ICD-10	Ph 1	Ph 2	Ph 3	Ph 4	Other	Total
Leukemia	D007938	—	C95	1	3	—	—	—	3
Myelodysplastic syndromes	D009190	—	D46	1	3	—	—	—	3
Myeloid leukemia acute	D015470	—	C92.0	1	3	—	—	—	3
Precursor cell lymphoblastic leukemia-lymphoma	D054198	—	C91.0	1	3	—	—	—	3
Psoriasis	D011565	EFO_0000676	L40	—	2	—	—	—	2
Gastroparesis	D018589	EFO_1000948	K31.84	1	1	—	—	—	2
Non-hodgkin lymphoma	D008228	—	C85.9	—	2	—	—	—	2
Bcr-abl positive chronic myelogenous leukemia	D015464	EFO_0000340	—	—	2	—	—	—	2
Myeloid leukemia	D007951	—	C92	—	2	—	—	—	2
Infertility	D007246	EFO_0000545	—	1	1	—	—	—	1

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Indications Phases 1

Indication	MeSH	Ontology	ICD-10	Ph 1	Ph 2	Ph 3	Ph 4	Other	Total
Therapeutic equivalency	D013810	—	—	6	—	—	—	—	6
Hepatitis c	D006526	—	B19.2	1	—	—	—	—	1
Chronic hepatitis c	D019698	EFO_0004220	B18.2	1	—	—	—	—	1
Hepatitis	D006505	—	K75.9	1	—	—	—	—	1
Chronic hepatitis	D006521	—	K73.9	1	—	—	—	—	1
Hepatitis a	D006506	EFO_0007305	B15	1	—	—	—	—	1
Hepatocellular carcinoma	D006528	—	C22.0	1	—	—	—	—	1
Liver neoplasms	D008113	EFO_1001513	C22.0	1	—	—	—	—	1
Anorexia	D000855	—	R63.0	1	—	—	—	—	1
Dyslipidemias	D050171	—	—	1	—	—	—	—	1

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Indications Without Phase

Indication	MeSH	Ontology	ICD-10	Ph 1	Ph 2	Ph 3	Ph 4	Other	Total
Sepsis	D018805	EFO_0001420	A41.9	—	—	—	—	1	1
Ischemic stroke	D000083242	—	—	—	—	—	—	1	1
Pancreatic neoplasms	D010190	EFO_0003860	C25	—	—	—	—	1	1
Vascular stiffness	D059289	—	—	—	—	—	—	1	1
Physiological phenomena	D010829	—	—	—	—	—	—	1	1
Morbid obesity	D009767	EFO_0001074	—	—	—	—	—	1	1
Angioedema	D000799	EFO_0005532	T78.3	—	—	—	—	1	1
Randomized controlled trials as topic	D016032	—	—	—	—	—	—	1	1
Endoplasmic reticulum stress	D059865	EFO_1001886	—	—	—	—	—	1	1
Exocrine pancreatic insufficiency	D010188	—	K86.81	—	—	—	—	1	1

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Epidemiology

Epidemiological information for investigational and approved indications

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Drug

General

Drug common name	Sitagliptin
INN	sitagliptin
Description	Sitagliptin is a triazolopyrazine that exhibits hypoglycemic activity. It has a role as a serine proteinase inhibitor, a hypoglycemic agent, an EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor, an environmental contaminant and a xenobiotic. It is a triazolopyrazine and a trifluorobenzene.
Classification	Small molecule
Drug class	dipeptidyl aminopeptidase-IV inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)	N[C@@H](CC(=O)N1CCn2c(nnc2C(F)(F)F)C1)Cc1cc(F)c(F)cc1F

Identifiers

PDB	—
CAS-ID	486460-32-6
RxCUI	—
ChEMBL ID	CHEMBL1422
ChEBI ID	40237
PubChem CID	4369359
DrugBank	DB01261
UNII ID	QFP0P1DV7Z (ChemIDplus, GSRS)

Target

Agency Approved

DPP4

Organism

Homo sapiens

Gene name

DPP4

Gene synonyms

ADCP2, CD26

NCBI Gene ID

1803

Protein name

dipeptidyl peptidase 4

Protein synonyms

ADABP, ADCP-2, Adenosine deaminase complexing protein 2, CD26, Dipeptidyl peptidase IV, dipeptidylpeptidase 4, dipeptidylpeptidase IV (CD26, adenosine deaminase complexing protein 2), DPP IV, Gly-Pro naphthylamidase, Post-proline dipeptidyl aminopeptidase IV, T-cell activation antigen CD26, TP103, Xaa-Pro-dipeptidylaminopeptidase

Uniprot ID

Q53TN1

Mouse ortholog

Dpp4 (13482)

dipeptidyl peptidase 4 (Q3U514)

Alternate

No data

Variants

No data

Financial

Revenue by drug

€

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Januvia – Merck & Co

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Janumet – Merck & Co

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Estimated US medical usage

Sitagliptin

Metformin

Total medical expenditures per year (USD, in millions)

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Number of persons purchased

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Sitagliptin

Total medical expenditures per year (USD, in millions)

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Number of persons purchased

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Number of purchases

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Trends

PubMed Central

Top Terms for Disease or Syndrome:

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Safety

Black-box Warning

Black-box warning for: Janumet, Sitagliptin and metformin hydrochloride, Zituvimet, Zituvimet xr

Adverse Events

Top Adverse Reactions

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48,948 adverse events reported

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