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Also known as: 668270-12-0, Tradjenta, Bi 1356, Bi-1356, Ondero, Linagliptin (bi-1356)
Molecular Formula
C25H28N8O2
Molecular Weight
472.5  g/mol
InChI Key
LTXREWYXXSTFRX-QGZVFWFLSA-N
FDA UNII
3X29ZEJ4R2

Linagliptin
A purine and quinazoline derivative that functions as an INCRETIN and DIPEPTIDYL-PEPTIDASE IV INHIBTOR. It is used as a HYPOGLYCEMIC AGENT in the treatment of TYPE II DIABETES MELLITUS.
Linagliptin is a Dipeptidyl Peptidase 4 Inhibitor. The mechanism of action of linagliptin is as a Dipeptidyl Peptidase 4 Inhibitor.
1 2D Structure

Linagliptin

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
2.1.2 InChI
InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1
2.1.3 InChI Key
LTXREWYXXSTFRX-QGZVFWFLSA-N
2.1.4 Canonical SMILES
CC#CCN1C2=C(N=C1N3CCCC(C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
2.1.5 Isomeric SMILES
CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
2.2 Other Identifiers
2.2.1 UNII
3X29ZEJ4R2
2.3 Synonyms
2.3.1 MeSH Synonyms

1. (r)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione

2. 1356, Bi

3. 1h-purine-2,6-dione, 8-((3r)-3-amino-1-piperidinyl)-7-(2-butynyl)-3,7-dihydro-3-methyl-1-((4-methyl-2-quinazolinyl)methyl)-

4. Bi 1356

5. Bi-1356

6. Bi1356

7. Tradjenta

8. Trajenta

2.3.2 Depositor-Supplied Synonyms

1. 668270-12-0

2. Tradjenta

3. Bi 1356

4. Bi-1356

5. Ondero

6. Linagliptin (bi-1356)

7. Trajenta

8. Trazenta

9. Bi-1356-bs

10. Bs 1356 Bs

11. Ione

12. 3x29zej4r2

13. Chembl237500

14. (r)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione

15. Bi-1356bs

16. Chebi:68610

17. Bi 1356 Bs

18. Bs-1356-bs

19. (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1h-purine-2,6(3h,7h)-dione

20. (r)-8-(3-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methylquinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione

21. 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-dione

22. 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione

23. 8-[(3r)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3- Methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-dione

24. 8-[(3r)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-dione

25. C25h28n8o2

26. Unii-3x29zej4r2

27. Linaglitpin

28. Linagliptin [usan:inn:jan]

29. Hsdb 8204

30. Tradjenta (tn)

31. 8-((3r)-3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1h-purine-2,6-dione

32. 8-[(3r)-3-amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1h-purine-2,6-dione

33. Linagliptin [mi]

34. Linagliptin [inn]

35. Linagliptin [jan]

36. Linagliptin [usan]

37. Linagliptin [vandf]

38. Linagliptin [mart.]

39. Linagliptin [who-dd]

40. Mls006010217

41. Schembl160188

42. Linagliptin (jan/usan/inn)

43. Gtpl6318

44. Amy8953

45. Ex-a076

46. Linagliptin [orange Book]

47. Bcpp000185

48. Dtxsid201021653

49. Bcp02462

50. Zinc3820029

51. Bdbm50228403

52. Glyxambi Component Linagliptin

53. Mfcd14635356

54. S3031

55. Akos015951179

56. Akos015995251

57. Ac-8761

58. Bcp9000854

59. Ccg-269463

60. Cs-0637

61. Db08882

62. Linagliptin Component Of Glyxambi

63. Trijardy Xr Component Linagliptin

64. Ncgc00346655-01

65. Ncgc00346655-02

66. 1h-purine-2,6-dione, 8-((3r)-3-amino-1-piperidinyl)-7-(2-butynyl)-3,7-dihydro-3-methyl-1-((4-methyl-2-quinazolinyl)methyl)-

67. As-35080

68. Bl164627

69. Hy-10284

70. Jentadueto Component Of Linagliptin

71. Linagliptin Component Of Jentadueto

72. Smr004701306

73. Linagliptin Component Of Trijardy Xr

74. Sw219813-1

75. D09566

76. Ab01563307_01

77. Ab01563307_03

78. 270l120

79. Q909745

80. J-519354

81. (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1h-purine-2,6(3h,7h)-dione

82. (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1h-purine-2,6-dione

83. 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(r)-aminopiperidin-1-yl)xanthine

84. 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(r)aminopiperidin-1-yl)xanthine

85. 1-[(4-methyl-quinazolin-2yl) Methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(r) Amino-piperidin-1-yl]-xanthine

86. 1-[(4-methylquinazolin-2-yl)-methyl]-3-methyl-7-(2-butin-1-yl)-8-(3-(r)-aminopiperidin-1-yl)-xanthine

87. 1-[(4-methylquinazolin-2-yl)methyl]-3-methyl-7-(2-butin-1-yl)-8-(3-(r)-aminopiperidin-1-yl)-xanthine

88. 1233245-11-8

89. 1h-purine-2,6-dione, 8-((3r)-3-amino-1-piperidinyl)-7-(2-butynyl)-3,7-dihydro-3-methyl-1-((4-methyl-2- Quinazolinyl)methyl)-

90. 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-d

91. 8-[(3r)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1h-purine-2,6-d Ione

92. Linagliptin; (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1h-purine-2,6(3h,7h)-dione

2.4 Create Date
2006-10-25
3 Chemical and Physical Properties
Molecular Weight 472.5 g/mol
Molecular Formula C25H28N8O2
XLogP31.9
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count7
Rotatable Bond Count4
Exact Mass472.23352217 g/mol
Monoisotopic Mass472.23352217 g/mol
Topological Polar Surface Area114 Ų
Heavy Atom Count35
Formal Charge0
Complexity885
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 2  
Drug NameTradjenta
PubMed HealthLinagliptin (By mouth)
Drug ClassesHypoglycemic
Drug LabelTRADJENTA (linagliptin) tablets contain, as the active ingredient, an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Linagliptin is described chemically as 1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,...
Active IngredientLinagliptin
Dosage FormTablet
RouteOral
Strength5mg
Market StatusPrescription
CompanyBoehringer Ingelheim

2 of 2  
Drug NameTradjenta
PubMed HealthLinagliptin (By mouth)
Drug ClassesHypoglycemic
Drug LabelTRADJENTA (linagliptin) tablets contain, as the active ingredient, an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Linagliptin is described chemically as 1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,...
Active IngredientLinagliptin
Dosage FormTablet
RouteOral
Strength5mg
Market StatusPrescription
CompanyBoehringer Ingelheim

4.2 Therapeutic Uses

Hypoglycemic Agents

National Library of Medicine's Medical Subject Headings. Linagliptin. Online file (MeSH, 2014). Available from, as of July 18, 2014: https://www.nlm.nih.gov/mesh/2014/mesh_browser/MBrowser.html


Tradjenta tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. /Included in US product label/

NIH; DailyMed. Current Medication Information for Tradjenta (Linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of July 18, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


4.3 Drug Warning

/BOXED WARNING/ WARNING: RISK OF LACTIC ACIDOSIS. Lactic acidosis is a rare, but serious, complication that can occur due to metformin accumulation. The risk increases with conditions such as renal impairment, sepsis, dehydration, excess alcohol intake, hepatic impairment, and acute congestive heart failure. The onset is often subtle, accompanied only by nonspecific symptoms such as malaise, myalgias, respiratory distress, increasing somnolence, and nonspecific abdominal distress. Laboratory abnormalities include low pH, increased anion gap, and elevated blood lactate. If acidosis is suspected, Jentadueto should be discontinued and the patient hospitalized immediately. /Linagliptin and metformin hydrochloride combination product/

NIH; DailyMed. Current Medication Information for Jentadueto (Linagliptin and Metformin Hydrochloride) Tablets (Revised: May 2014). Available from, as of July 18, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=f6dd9b86-0d18-95d4-2bc7-05591bfdd597


FDA is evaluating unpublished new findings by a group of academic researchers that suggest an increased risk of pancreatitis and pre-cancerous cellular changes called pancreatic duct metaplasia in patients with type 2 diabetes treated with a class of drugs called incretin mimetics. These findings were based on examination of a small number of pancreatic tissue specimens taken from patients after they died from unspecified causes. FDA has asked the researchers to provide the methodology used to collect and study these specimens and to provide the tissue samples so the Agency can further investigate potential pancreatic toxicity associated with the incretin mimetics. Drugs in the incretin mimetic class include exenatide (Byetta, Bydureon), liraglutide (Victoza), sitagliptin (Januvia, Janumet, Janumet XR, Juvisync), saxagliptin (Onglyza, Kombiglyze XR), alogliptin (Nesina, Kazano, Oseni), and linagliptin (Tradjenta, Jentadueto). These drugs work by mimicking the incretin hormones that the body usually produces naturally to stimulate the release of insulin in response to a meal. They are used along with diet and exercise to lower blood sugar in adults with type 2 diabetes. FDA has not reached any new conclusions about safety risks with incretin mimetic drugs. This early communication is intended only to inform the public and health care professionals that the Agency intends to obtain and evaluate this new information. ... FDA will communicate its final conclusions and recommendations when its review is complete or when the Agency has additional information to report. The Warnings and Precautions section of drug labels and patient Medication Guides for incretin mimetics contain warnings about the risk of acute pancreatitis. FDA has not previously communicated about the potential risk of pre-cancerous findings of the pancreas with incretin mimetics. FDA has not concluded these drugs may cause or contribute to the development of pancreatic cancer. At this time, patients should continue to take their medicine as directed until they talk to their health care professional, and health care professionals should continue to follow the prescribing recommendations in the drug labels. ...

US FDA; Safety Alerts for Human Medicial Products: Incretin Mimetic Drugs for Type 2 Diabetes: Early Communication - Reports of Possible Increased Risk of Pancreatitis and Pre-cancerous Findings of the Pancreas (Posted March 14, 1013). Available from, as of August 1, 2014: https://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm343805.htm


There have been postmarketing reports of acute pancreatitis, including fatal pancreatitis, in patients taking Tradjenta. Take careful notice of potential signs and symptoms of pancreatitis. If pancreatitis is suspected, promptly discontinue Tradjenta and initiate appropriate management. It is unknown whether patients with a history of pancreatitis are at increased risk for the development of pancreatitis while using Tradjenta.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


There have been postmarketing reports of serious hypersensitivity reactions in patients treated with Tradjenta. These reactions include anaphylaxis, angioedema, and exfoliative skin conditions. Onset of these reactions occurred within the first 3 months after initiation of treatment with Tradjenta, with some reports occurring after the first dose. If a serious hypersensitivity reaction is suspected, discontinue Tradjenta, assess for other potential causes for the event, and institute alternative treatment for diabetes. Angioedema has also been reported with other dipeptidyl peptidase-4 (DPP-4) inhibitors. Use caution in a patient with a history of angioedema to another DPP-4 inhibitor because it is unknown whether such patients will be predisposed to angioedema with Tradjenta.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


For more Drug Warnings (Complete) data for Linagliptin (20 total), please visit the HSDB record page.


4.4 Drug Indication

Linagliptin is indicated for the treatment of type II diabetes in addition to diet and exercise. It should not be used to treat type I diabetes or in diabetic ketoacidosis. An extended-release combination product containing empagliflozin, linagliptin, and metformin was approved by the FDA in January 2020 for the improvement of glycemic control in adults with type 2 diabetes mellitus when used adjunctively with diet and exercise.


FDA Label


Trajenta is indicated in the treatment of type 2 diabetes mellitus to improve glycaemic control in adults:

as

* monotherapy:

- in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to intolerance, or contraindicated due to renal impairment.

as

* combination therapy:

- in combination with metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control.

- in combination with a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.

- in combination with insulin with or without metformin, when this regimen alone, with diet and exercise, does not provide adequate glycaemic control.


5 Pharmacology and Biochemistry
5.1 Pharmacology

A 5mg oral dose of linagliptin results in >80% inhibition of dipeptidyl peptidase 4 (DPP-4) for 24 hours. Inhibition of DPP-4 increases the concentration of glucagon-like peptide 1 (GLP-1), leading to decreased glycosylated hemoglobin and fasting plasma glucose.


5.2 MeSH Pharmacological Classification

Dipeptidyl-Peptidase IV Inhibitors

Compounds that suppress the degradation of INCRETINS by blocking the action of DIPEPTIDYL-PEPTIDASE IV. This helps to correct the defective INSULIN and GLUCAGON secretion characteristic of TYPE 2 DIABETES MELLITUS by stimulating insulin secretion and suppressing glucagon release. (See all compounds classified as Dipeptidyl-Peptidase IV Inhibitors.)


Hypoglycemic Agents

Substances which lower blood glucose levels. (See all compounds classified as Hypoglycemic Agents.)


Incretins

Peptides which stimulate INSULIN release from the PANCREATIC BETA CELLS following oral nutrient ingestion, or postprandially. (See all compounds classified as Incretins.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
LINAGLIPTIN
5.3.2 FDA UNII
3X29ZEJ4R2
5.3.3 Pharmacological Classes
Dipeptidyl Peptidase 4 Inhibitors [MoA]; Dipeptidyl Peptidase 4 Inhibitor [EPC]
5.4 ATC Code

A10BH05


A - Alimentary tract and metabolism

A10 - Drugs used in diabetes

A10B - Blood glucose lowering drugs, excl. insulins

A10BH - Dipeptidyl peptidase 4 (dpp-4) inhibitors

A10BH05 - Linagliptin


5.5 Absorption, Distribution and Excretion

Absorption

Oral bioavailability of linagliptin is 30%.


Route of Elimination

84.7% of linagliptin is eliminated in the feces and 5.4% is eliminated in the urine.


Volume of Distribution

A single intravenous dose of 5mg results in a volume of distribution of 1110L. However an intravenous infusion of 0.5-10mg results in a volume of distribution of 380-1540L.


Clearance

Total clearance of linagliptin is 374mL/min.


Available animal data have shown excretion of linagliptin in milk at a milk-to-plasma ratio of 4:1.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


After oral administration of a single 5-mg dose to healthy subjects, peak plasma concentrations of linagliptin occurred at approximately 1.5 hours post dose (Tmax); the mean plasma area under the curve (AUC) was 139 nmol*h/L and maximum concentration (Cmax) was 8.9 nmol/L.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


The absolute bioavailability of linagliptin is approximately 30%. High-fat meal reduced Cmax by 15% and increased AUC by 4%; this effect is not clinically relevant. Tradjenta may be administered with or without food.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


Following administration of an oral (14C)-linagliptin dose to healthy subjects, approximately 85% of the administered radioactivity was eliminated via the enterohepatic system (80%) or urine (5%) within 4 days of dosing. Renal clearance at steady state was approximately 70 mL/min.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


For more Absorption, Distribution and Excretion (Complete) data for Linagliptin (6 total), please visit the HSDB record page.


5.6 Metabolism/Metabolites

An oral dose of linagliptin is excreted primarily in the feces. 90% of an oral dose is excreted unchanged in the urine and feces. The predominant metabolite in the plasma is CD1790 and the predominant metabolite recovered after excretion was M489(1). Other metabolites are produced through oxidation, oxidative degradation, N-acetylation, glucuronidation, and cysteine adduct formation. Other metabolites have been identified through mass spectrometry though no structures were determined. Metabolism of linagliptin is mediated by cytochrome P450 3A4, aldo-keto reductases, and carbonyl reductases.


Following oral administration, the majority (about 90%) of linagliptin is excreted unchanged, indicating that metabolism represents a minor elimination pathway. A small fraction of absorbed linagliptin is metabolized to a pharmacologically inactive metabolite, which shows a steady-state exposure of 13.3% relative to linagliptin.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


5.7 Biological Half-Life

The terminal half life of linagliptin is 155 hours.


The effective half-life for accumulation of linagliptin, as determined from oral administration of multiple doses of linagliptin 5 mg, is approximately 12 hours.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


Plasma concentrations of linagliptin decline in at least a biphasic manner with a long terminal half-life (>100 hours), related to the saturable binding of linagliptin to DPP-4.

NIH; DailyMed. Current Medication Information for Tradjenta (linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of August 1, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


5.8 Mechanism of Action

Linagliptin is a competitive, reversible DPP-4 inhibitor. Inhibition of this enzyme slows the breakdown of GLP-1 and glucose-dependant insulinotropic polypeptide (GIP). GLP-1 and GIP stimulate the release of insulin from beta cells in the pancreas while inhibiting release of glucagon from pancreatic beta cells. These effects together reduce the breakdown of glycogen in the liver and increase insulin release in response to glucose.


Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta-cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha-cells, resulting in a reduction in hepatic glucose output.

NIH; DailyMed. Current Medication Information for Tradjenta (Linagliptin) Tablet, Film-coated (Revised: June 2014). Available from, as of July 31, 2014: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f


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Rochem International Inc

U.S.A

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Virtual BoothRochem, your partner in developing, sourcing, and supplying pharmaceutical & animal health ingredients of Chinese origin.

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Suanfarma

Spain

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Virtual BoothSuanFarma is present in all origins: Natural, Chemical & Biotechnological.

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Dr. Reddy's Laboratories

India

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Virtual BoothDRL offers a portfolio of products & services, including APIs, CMO services, generics, biosimilars & differentiated formulations.

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Faran Shimi Pharmaceutical

Iran

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Virtual BoothFaran Shimi: Leading producer of high-quality APIs & alkaloid opiates, serving major pharmaceutical companies across the Middle East.

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Virupaksha Organics

India

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Aptra Synthesis

India

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Virtual BoothAptra Synthesis produces APIs, Pellets (Semi-finished Formulations), and Intermediates.

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Aptra Synthesis
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NASHIK, MAHARASHTRA.","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1725993000,"product":"LINAGLIPTIN IH(B\/N-LGI04-103774,LGS01-402561,3-BBL-000046,LG02-900298,LG04-P-600079,DMAL-000044,LG03-900299,LG04(S)-5028","address":"MOREPEN VILLAGE, NALAGARH ROAD,","city":"N\/A","supplier":"MOREPEN LABORATORIES","supplierCountry":"INDIA","foreign_port":"ATHENS","customer":"TO THE ORDER OF","customerCountry":"GREECE","quantity":"0.70","actualQuantity":"0.7","unit":"KGS","unitRateFc":"1900","totalValueFC":"1236","currency":"USD","unitRateINR":147966.57142857145,"date":"11-Sep-2024","totalValueINR":"103576.6","totalValueInUsd":"1236","indian_port":"Delhi Air","hs_no":"29420090","bill_no":"3933306","productDescription":"API","marketType":"REGULATED MARKET","country":"GREECE","selfForZScoreResived":"Pharma Grade","supplierPort":"Delhi Air","supplierAddress":"MOREPEN VILLAGE, NALAGARH ROAD,, N\/A","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1726511400,"product":"LINAGLIPTIN IN-HOUSE","address":"PLOT NO.131,3RD FLOOR,NARMADA","city":"HYDERABAD. AP","supplier":"OPTIMUS DRUGS PRIVATE ","supplierCountry":"INDIA","foreign_port":"CAIRO","customer":"M\/S P&C PELLETS & CR PRODUCT","customerCountry":"EGYPT","quantity":"20.00","actualQuantity":"20","unit":"KGS","unitRateFc":"800","totalValueFC":"15774.8","currency":"USD","unitRateINR":66097.399999999994,"date":"17-Sep-2024","totalValueINR":"1321948","totalValueInUsd":"15774.8","indian_port":"Hyderabad Air","hs_no":"29335990","bill_no":"4087329","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"EGYPT","selfForZScoreResived":"Pharma Grade","supplierPort":"Hyderabad Air","supplierAddress":"PLOT NO.131,3RD FLOOR,NARMADA, HYDERABAD. AP","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1726597800,"product":"LINAGLIPTIN (EXPORT INVOICE NO:6124010319 DT:06.09.2024)","address":"SYNO.257 258\/1, DNO.11-6\/56,","city":"VILLAGE BALANGAR POST HYDERABAD","supplier":"LEE PHARMA","supplierCountry":"INDIA","foreign_port":"SHEREMETYEVO","customer":"NAO SEVERNAYA ZVEZDA","customerCountry":"RUSSIA","quantity":"1.00","actualQuantity":"1","unit":"KGS","unitRateFc":"2800","totalValueFC":"2628.9","currency":"USD","unitRateINR":220308,"date":"18-Sep-2024","totalValueINR":"220308","totalValueInUsd":"2628.9","indian_port":"Hyderabad Air","hs_no":"29333200","bill_no":"4139888","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"RUSSIA","selfForZScoreResived":"Pharma Grade","supplierPort":"Hyderabad Air","supplierAddress":"SYNO.257 258\/1, DNO.11-6\/56,, VILLAGE BALANGAR POST HYDERABAD","customerAddress":""},{"dataSource":"API Import","activeIngredients":"","year":"2022","qtr":"Q1","strtotime":1645468200,"product":"LINAGLIPTIN (SEEDING MATERIAL)","address":"12th floor,Commerz II, International Business Park, Oberoi","city":"Goregaon East","supplier":"CHEMICAL INDUSTRIES ASSOCIATION","supplierCountry":"ISRAEL","foreign_port":"NA","customer":"TEVA API","customerCountry":"INDIA","quantity":"0.40","actualQuantity":"0.4","unit":"KGS","unitRateFc":"8000","totalValueFC":"3246.7","currency":"USD","unitRateINR":"608400","date":"22-Feb-2022","totalValueINR":"243360","totalValueInUsd":"3246.7","indian_port":"DELHI AIR","hs_no":"29335990","bill_no":"7599193","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"ISRAEL","selfForZScoreResived":"Pharma Grade","supplierPort":"NA","supplierAddress":"","customerAddress":"12th floor,Commerz II, International Business Park, Oberoi"},{"dataSource":"API Import","activeIngredients":"","year":"2022","qtr":"Q4","strtotime":1669746600,"product":"LINAGLIPTIN 5 MG AND METFORMIN HYDROCHLORIDE 1000 MG (EXTENDED RELEASE) TABLETS(90 TABLETS)(LOT #3208414)","address":"UNIT NO .3 ,CORPORATE PARK, SION TROMBAY ROAD, CHEMBUR","city":"MUMBAI","supplier":"GOOD HEALTH PHARMA ","supplierCountry":"UNITED STATES","foreign_port":"NA","customer":"ABBOTT LABORATORIES","customerCountry":"INDIA","quantity":"0.50","actualQuantity":"0.5","unit":"KGS","unitRateFc":"3040","totalValueFC":"2313.4","currency":"USD","unitRateINR":"377600.4","date":"30-Nov-2022","totalValueINR":"188800.2","totalValueInUsd":"2313.4","indian_port":"HYDERABAD AIR","hs_no":"29339990","bill_no":"3529515","productDescription":"API","marketType":"REGULATED MARKET","country":"UNITED STATES","selfForZScoreResived":"Pharma Grade","supplierPort":"NA","supplierAddress":"","customerAddress":"UNIT NO .3 ,CORPORATE PARK, SION TROMBAY ROAD, CHEMBUR"},{"dataSource":"API Import","activeIngredients":"","year":"2023","qtr":"Q2","strtotime":1685989800,"product":"LINAGLIPTIN. B\/N: D5425-23-001 (2.5 KG) & MFG. DT. 20\/04\/23B\/N: D5425-23-002M1 (2.5 KG) MFG. DT. 21\/04\/23 RETEST DT. 03","address":"UNISON HOUSE, NR. PRERNATIRTH DER NR. RATNADEEP-2, SATELLITE, JODHPUR","city":"AHMEDABAD","supplier":"ZHEJIANG HUAHAI PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"NA","customer":"UNISON PHARMACEUTICALS PRIVATE LIMITED","customerCountry":"INDIA","quantity":"5.00","actualQuantity":"5","unit":"KGS","unitRateFc":"2500","totalValueFC":"12683.1","currency":"USD","unitRateINR":"208499.9","date":"06-Jun-2023","totalValueINR":"1042500.333","totalValueInUsd":"12683.1","indian_port":"AHMEDABAD AIR","hs_no":"29334900","bill_no":"0","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"NA","supplierAddress":"","customerAddress":"UNISON HOUSE, NR. PRERNATIRTH DER NR. RATNADEEP-2, SATELLITE, JODHPUR"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q1","strtotime":1710786600,"product":"LINAGLIPTIN (REJECTED MATERIAL VIDE SB NO-4000809 DT:09.10.2023,RID NO-252303870604)","address":"8-3-166\/7\/1, HETERO HOUSE,","city":"HYDERABAD, AP.","supplier":"XXNG XX COXXHANXXHU XXG MXX VIXX UY","supplierCountry":"VIETNAM","foreign_port":"HO CHI MINH CITY","customer":"HONOUR LAB LTD","customerCountry":"INDIA","quantity":"4.00","actualQuantity":"4","unit":"KGS","unitRateFc":"3385.4","totalValueFC":"13682.7","currency":"USD","unitRateINR":"284038.3","date":"19-Mar-2024","totalValueINR":"1136153","totalValueInUsd":"13682.7","indian_port":"Vizag-HIPL SEZ","hs_no":"29339990","bill_no":"1000161","productDescription":"API","marketType":"LESS REGULATED MARKET","country":"VIETNAM, DEMOCRA","selfForZScoreResived":"Pharma Grade","supplierPort":"HO CHI MINH CITY","supplierAddress":"N\/A","customerAddress":"8-3-166\/7\/1, HETERO HOUSE,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1721413800,"product":"LINAGLIPTIN. B\/N: D5425-23-004M1 MFG. DT. 04\/06\/2023 RETESTDT. 05\/2028.","address":"PLOT NO.5222, PHASE- IV,","city":"AHMEDABAD -","supplier":"ZHEJIANG HUAHAI PHARMACEUTICAL","supplierCountry":"CHINA","foreign_port":"HANGCHOW (HANGZHOU)","customer":"UNISON PHARMACEUTICALS PRIVATE LIMITED","customerCountry":"INDIA","quantity":"0.80","actualQuantity":"0.8","unit":"KGS","unitRateFc":"2500","totalValueFC":"2022.9","currency":"USD","unitRateINR":"211375","date":"20-Jul-2024","totalValueINR":"169100","totalValueInUsd":"2022.9","indian_port":"Ahmedabad Air","hs_no":"29334900","bill_no":"4613450","productDescription":"API","marketType":"REGULATED MARKET","country":"CHINA","selfForZScoreResived":"Pharma Grade","supplierPort":"HANGCHOW (HANGZHOU)","supplierAddress":"XUNQIAO,LINHAI ,ZHEJIANG 317024 CHISDNF CHINA","customerAddress":"PLOT NO.5222, PHASE- IV,"}]
04-Jan-2021
18-Sep-2024
KGS
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Average Price (USD/KGS)

Number of Transactions

Total Quantity (KGS)

Total Value (USD)

Quantity (KGS) & Unit rate (USD/KGS) over time

API Imports and Exports

Importing Country Total Quantity
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(USD/KGS)
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INTERMEDIATES SUPPLIERS

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01

2024 ACI Convention
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Virtual BoothFaran Shimi: Leading producer of high-quality APIs & alkaloid opiates, serving major pharmaceutical companies across the Middle East.

CAS Number : 309956-78-3

End Use API : Linagliptin

About The Company : Faran Shimi Pharmaceutical Company, established in 2001 and affiliated with Golrang Pharmaceutical Investment Co, manufactures high-quality Active Pharmaceutica...

Faran Shimi Pharmaceutical

02

2024 ACI Convention
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Virtual BoothFaran Shimi: Leading producer of high-quality APIs & alkaloid opiates, serving major pharmaceutical companies across the Middle East.

CAS Number : 853029-57-9

End Use API : Linagliptin

About The Company : Faran Shimi Pharmaceutical Company, established in 2001 and affiliated with Golrang Pharmaceutical Investment Co, manufactures high-quality Active Pharmaceutica...

Faran Shimi Pharmaceutical

03

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Virtual BoothWith Virupaksha, you get a quality product with on-time delivery.

CAS Number : 109113-72-6

End Use API : Linagliptin

About The Company : Virupaksha Organics, founded in 2003 by G. Chandra Mouliswar Reddy, is committed to delivering products of the utmost quality to its customers. In a span of les...

Virupaksha

04

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Virtual BoothWith Virupaksha, you get a quality product with on-time delivery.

CAS Number : 666816-98-4

End Use API : Linagliptin

About The Company : Virupaksha Organics, founded in 2003 by G. Chandra Mouliswar Reddy, is committed to delivering products of the utmost quality to its customers. In a span of les...

Virupaksha

05

  • fda
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Virtual BoothWith Virupaksha, you get a quality product with on-time delivery.

CAS Number : 309956-78-3

End Use API : Linagliptin

About The Company : Virupaksha Organics, founded in 2003 by G. Chandra Mouliswar Reddy, is committed to delivering products of the utmost quality to its customers. In a span of les...

Virupaksha

06

  • fda
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Virtual BoothTagoor's product development expertise, backed by our comprehensive understanding of the processes, helps us offer high-quality APIs.

CAS Number : 309956-78-3

End Use API : Linagliptin

About The Company : Tagoor Laboratories, established in 2018, is a part of the Tagoor Group. It specializes in providing APIs, advanced intermediates and key starting materials for...

Tagoor Laboratories

07

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Virtual BoothTagoor's product development expertise, backed by our comprehensive understanding of the processes, helps us offer high-quality APIs.

CAS Number : 334618-23-4

End Use API : Linagliptin

About The Company : Tagoor Laboratories, established in 2018, is a part of the Tagoor Group. It specializes in providing APIs, advanced intermediates and key starting materials for...

Tagoor Laboratories

08

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Virtual BoothTagoor's product development expertise, backed by our comprehensive understanding of the processes, helps us offer high-quality APIs.

CAS Number : 309956-78-3

End Use API : Linagliptin

About The Company : Tagoor Laboratories, established in 2018, is a part of the Tagoor Group. It specializes in providing APIs, advanced intermediates and key starting materials for...

Tagoor Laboratories

09

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Virtual BoothTagoor's product development expertise, backed by our comprehensive understanding of the processes, helps us offer high-quality APIs.

CAS Number : 334618-23-4

End Use API : Linagliptin

About The Company : Tagoor Laboratories, established in 2018, is a part of the Tagoor Group. It specializes in providing APIs, advanced intermediates and key starting materials for...

Tagoor Laboratories

10

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Virtual BoothTagoor's product development expertise, backed by our comprehensive understanding of the processes, helps us offer high-quality APIs.

CAS Number : 309956-78-3

End Use API : Linagliptin

About The Company : Tagoor Laboratories, established in 2018, is a part of the Tagoor Group. It specializes in providing APIs, advanced intermediates and key starting materials for...

Tagoor Laboratories
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Europe

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01

SupplySide West 2024
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Several substances refer to content

Brand Name : Jentadueto

Dosage Form : FILM COATED PILL

Dosage Strength : 2.5 MG / 1000 MG

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Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

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02

SupplySide West 2024
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linagliptin

Brand Name : Trajenta

Dosage Form : FILM COATED PILL

Dosage Strength : 5 MG

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Registration Country : Sweden

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Metformin; Linagliptin

Brand Name : Jentadueto

Dosage Form : Metformin+Linagliptin+2,51,000 Mg 56 Combined Oral Use

Dosage Strength : 56 cpr riv 2.5 mg + 1,000 mg

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Regulatory Info :

Registration Country : Italy

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04

SupplySide West 2024
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Linagliptin

Brand Name : Trajenta

Dosage Form : Antic-calc Tablet, Film Coated

Dosage Strength : 5 mg

Packaging : Blister

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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05

SupplySide West 2024
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Linagliptin

Brand Name : Trajenta

Dosage Form : Antic-calc Tablet, Film Coated

Dosage Strength : 5 mg

Packaging : Blister

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Application Number :

Regulatory Info :

Registration Country : Norway

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06

SupplySide West 2024
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Metformin; Linagliptin

Brand Name : Jentadueto

Dosage Form : Antic-calc Tablet, Film Coated

Dosage Strength : 2.5MG; 850MG

Packaging : Blister, endose

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Application Number :

Regulatory Info :

Registration Country : Norway

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07

SupplySide West 2024
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Empagliflozinum; Linagliptinum

Brand Name : Glyxambi

Dosage Form : Filmtabl

Dosage Strength : 10mg/5mg

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Regulatory Info :

Registration Country : Switzerland

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SupplySide West 2024
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Empagliflozinum; Linagliptinum

Brand Name : Glyxambi

Dosage Form : Filmtabl

Dosage Strength : 10mg/5mg

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Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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SupplySide West 2024
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Linagliptin; Metformin hydrochloride

Brand Name : Jentadueto

Dosage Form : Filmtabl

Dosage Strength : 2.5mg/1000mg

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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10

SupplySide West 2024
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Linagliptin; Metformin hydrochloride

Brand Name : Jentadueto

Dosage Form : Filmtable

Dosage Strength : 2.5mg/500mg

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Switzerland

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DRUG PRODUCT COMPOSITIONS

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DOSAGE - TABLET;ORAL - 5MG

USFDA APPLICATION NUMBER - 201280

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DOSAGE - TABLET;ORAL - 2.5MG;1GM

USFDA APPLICATION NUMBER - 201281

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DOSAGE - TABLET;ORAL - 2.5MG;500MG

USFDA APPLICATION NUMBER - 201281

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DOSAGE - TABLET;ORAL - 2.5MG;850MG

USFDA APPLICATION NUMBER - 201281

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DOSAGE - TABLET;ORAL - 10MG;5MG

USFDA APPLICATION NUMBER - 206073

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DOSAGE - TABLET;ORAL - 25MG;5MG

USFDA APPLICATION NUMBER - 206073

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Virtual BoothNanjing Well is focused on R&D, production & sales of Pharmaceutical Excipients & Synthetic Lubricating base oils.

08

Finar

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