Finished Dosage Form (FDF) import of Xanomeline obtained from Indian Custom Trade Statistics

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Chemistry

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Also known as: 131986-45-3, 3-(hexyloxy)-4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazole, Ly 246708, Ly-246708, Ly246708, 3-hexoxy-4-(1-methyl-3,6-dihydro-2h-pyridin-5-yl)-1,2,5-thiadiazole
Molecular Formula
C14H23N3OS
Molecular Weight
281.42  g/mol
InChI Key
JOLJIIDDOBNFHW-UHFFFAOYSA-N
FDA UNII
9ORI6L73CJ

Xanomeline
Xanomeline is under investigation in clinical trial NCT02831231 (Pilot Study Comparing Effects of Xanomeline Alone to Xanomeline Plus Trospium).
1 2D Structure

Xanomeline

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole
2.1.2 InChI
InChI=1S/C14H23N3OS/c1-3-4-5-6-10-18-14-13(15-19-16-14)12-8-7-9-17(2)11-12/h8H,3-7,9-11H2,1-2H3
2.1.3 InChI Key
JOLJIIDDOBNFHW-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CCCCCCOC1=NSN=C1C2=CCCN(C2)C
2.2 Other Identifiers
2.2.1 UNII
9ORI6L73CJ
2.3 Synonyms
2.3.1 MeSH Synonyms

1. (3-o-hexyloxy)-tztp

2. 3-(3-o-hexyl-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine

3. Ly 246708

4. Ly-246708

5. Ly246708

6. Xanomeline Tartrate

2.3.2 Depositor-Supplied Synonyms

1. 131986-45-3

2. 3-(hexyloxy)-4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazole

3. Ly 246708

4. Ly-246708

5. Ly246708

6. 3-hexoxy-4-(1-methyl-3,6-dihydro-2h-pyridin-5-yl)-1,2,5-thiadiazole

7. 9ori6l73cj

8. Chembl21536

9. 5-(4-hexyloxy-[1,2,5]thiadiazol-3-yl)-1-methyl-1,2,3,6-tetrahydro-pyridine

10. Chebi:10056

11. Ly-246708 Free Base

12. 5-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1-methyl-1,2,3,6-tetrahydropyridine

13. Xanomeline (usan)

14. Xanomeline [usan]

15. Pyridine, 3-(4-(hexyloxy)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methyl-

16. Xanomeline [usan:inn]

17. Unii-9ori6l73cj

18. Lumeron

19. Memcor

20. Hexyloxy-tztp

21. Pyridine, 3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methyl-

22. Xanomeline [mi]

23. Xanomeline [inn]

24. Gtpl57

25. 3-(4-(hexyloxy)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyridine

26. Xanomeline [mart.]

27. Xanomeline [who-dd]

28. Schembl121046

29. Dtxsid60157286

30. Bcp31492

31. Ex-a6592

32. Zinc1532358

33. Bdbm50003359

34. Mfcd00867179

35. Akos016007489

36. Db15357

37. Sb18821

38. Nnc-11-0232

39. Ds-15663

40. Hy-105182

41. Cs-0025224

42. Ft-0602214

43. C72296

44. D06330

45. A888347

46. L000694

47. Q8042940

48. Ly-246708; Ly246708; Ly 246708

49. 3-(4-hexoxy-1,2,5-thiadiazol-3-yl)-1-methyl-5,6-dihydro-2h-pyridine

50. 3-(4-hexyloxy-1 ,2,5-thiadiazol-3-yl)-1 ,2,5,6-tetrahydro-1-methyl-pyridine

51. 5-(4-hexyloxy-[1,2,5]thiadiazol-3-yl)-1-methyl-1,2,3,6-tetrahydro-pyridine; Oxalic Acid

52. 5-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1-methyl-1,2,3,6-tetrahydropyridine, Aldrichcpr

53. 1018845-70-9

2.4 Create Date
2005-06-24
3 Chemical and Physical Properties
Molecular Weight 281.42 g/mol
Molecular Formula C14H23N3OS
XLogP33.3
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count5
Rotatable Bond Count7
Exact Mass281.15618354 g/mol
Monoisotopic Mass281.15618354 g/mol
Topological Polar Surface Area66.5 Ų
Heavy Atom Count19
Formal Charge0
Complexity298
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Pharmacology and Biochemistry
4.1 MeSH Pharmacological Classification

Muscarinic Agonists

Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate. (See all compounds classified as Muscarinic Agonists.)


Parasympathomimetics

Drugs that mimic the effects of parasympathetic nervous system activity. Included here are drugs that directly stimulate muscarinic receptors and drugs that potentiate cholinergic activity, usually by slowing the breakdown of acetylcholine (CHOLINESTERASE INHIBITORS). Drugs that stimulate both sympathetic and parasympathetic postganglionic neurons (GANGLIONIC STIMULANTS) are not included here. (See all compounds classified as Parasympathomimetics.)


Psychotropic Drugs

A loosely defined grouping of drugs that have effects on psychological function. Here the psychotropic agents include the antidepressive agents, hallucinogens, and tranquilizing agents (including the antipsychotics and anti-anxiety agents). (See all compounds classified as Psychotropic Drugs.)


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XANOMELINE TARTRATE

NDC Package Code : 58032-3003

Start Marketing Date : 2023-03-17

End Marketing Date : 2025-12-31

Dosage Form (Strength) : POWDER (1kg/kg)

Marketing Category : BULK INGREDIENT

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[{"dataSource":"API Export","activeIngredients":"","year":"2021","qtr":"Q2","strtotime":1623954600,"product":"XANOMELINE TARTRATE","address":"FLAT NO.204,IIND FLOOR,MERIDIANPLAZA,6-3-853\/1,AMEERPET,","city":"HYDERABAD-ANDHRA PRADESH.","supplier":"NEULAND LABORATORIES","supplierCountry":"INDIA","foreign_port":"BOSTON - LOGAN MA","customer":"MASY BIOSERVICES","customerCountry":"UNITED STATES","quantity":"129.90","actualQuantity":"129.9","unit":"KGS","unitRateFc":"2527.8","totalValueFC":"321678.3","currency":"USD","unitRateINR":182125,"date":"18-Jun-2021","totalValueINR":"23658037.5","totalValueInUsd":"321678.3","indian_port":"HYDERABAD AIR","hs_no":"29181390","bill_no":"2523111","productDescription":"API","marketType":"REGULATED MARKET","country":"UNITED STATES","selfForZScoreResived":"Pharma Grade","supplierPort":"HYDERABAD AIR","supplierAddress":"FLAT NO.204,IIND FLOOR,MERIDIANPLAZA,6-3-853\/1,AMEERPET,, HYDERABAD-ANDHRA PRADESH.","customerAddress":""},{"dataSource":"API Export","activeIngredients":"","year":"2022","qtr":"Q1","strtotime":1643567400,"product":"XANOMELINE TARTRATE (QTY:570.910 KGS)","address":"SANALI INFO PARK, 8-2-120\/113,ROAD NO.2, BANJARA HILLS","city":"HYDERABAD,TELANGANA","supplier":"NEULAND LABORATORIES","supplierCountry":"INDIA","foreign_port":"NEW YORK - JOHN F. 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18-Jun-2021
15-Sep-2023
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Drugs in Development

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Details:

KarXT (xanomeline-trospium) is an oral, investigational M1/M4-preferring muscarinic agonist in development for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer’s disease.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable April 06, 2024

blank

01

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : KarXT (xanomeline-trospium) is an oral, investigational M1/M4-preferring muscarinic agonist in development for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer’s disease.

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : Not Applicable

April 06, 2024

blank

Details:

Through the acquisition, BMS will enhance the development of KarXT (xanomeline-trospium), an antipsychotic with a novel mechanism of being a first-in-class M1 / M4 muscarinic receptor agonist, with differentiated efficacy and safety for treating schizophrenia in adults.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Bristol Myers Squibb

Deal Size: $14,000.0 million Upfront Cash: $14,000.0 million

Deal Type: Acquisition March 18, 2024

blank

02

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : Through the acquisition, BMS will enhance the development of KarXT (xanomeline-trospium), an antipsychotic with a novel mechanism of being a first-in-class M1 / M4 muscarinic receptor agonist, with differentiated efficacy and safety for treating schizoph...

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : $14,000.0 million

March 18, 2024

blank

Details:

Through the acquisition, BMS will enhance the development of KarXT (xanomeline-trospium), an antipsychotic with a novel mechanism of being a first-in-class M1 / M4 muscarinic receptor agonist, with differentiated efficacy and safety for treating schizophrenia in adults.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Bristol Myers Squibb

Deal Size: $14,000.0 million Upfront Cash: $14,000.0 million

Deal Type: Acquisition December 22, 2023

blank

03

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : Through the acquisition, BMS will enhance the development of KarXT (xanomeline-trospium), an antipsychotic with a novel mechanism of being a first-in-class M1 / M4 muscarinic receptor agonist, with differentiated efficacy and safety for treating schizoph...

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : $14,000.0 million

December 22, 2023

blank

Details:

KarXT (xanomeline and trospium chloride) is an M1/M4 receptor Agonist small molecule drug delivered orally in capsule form for the treatment of Schizophrenia.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 29, 2023

blank

04

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : KarXT (xanomeline and trospium chloride) is an M1/M4 receptor Agonist small molecule drug delivered orally in capsule form for the treatment of Schizophrenia.

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 29, 2023

blank

Details:

KarXT (xanomeline-trospium) is an oral, investigational M1/M4-preferring muscarinic agonist in development for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer’s disease.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 17, 2023

blank

05

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : KarXT (xanomeline-trospium) is an oral, investigational M1/M4-preferring muscarinic agonist in development for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer’s disease.

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 17, 2023

blank

Details:

KarXT (xanomeline-trospium) is an oral, investigational M1/M4-preferring muscarinic agonist in development for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer’s disease.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 16, 2023

blank

06

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : KarXT (xanomeline-trospium) is an oral, investigational M1/M4-preferring muscarinic agonist in development for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer’s disease.

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : Not Applicable

November 16, 2023

blank

Details:

KarXT (xanomeline-trospium) is an oral, investigational M1/M4-preferring muscarinic agonist in development for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer’s disease.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Karuna Therapeutics

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable September 28, 2023

blank

07

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : KarXT (xanomeline-trospium) is an oral, investigational M1/M4-preferring muscarinic agonist in development for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer’s disease.

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : Not Applicable

September 28, 2023

blank

Details:

The proceedings will be used to fund Karuna's ongoing and planned clinical trials of KarXT (xanomeline), to support the potential commercialization of KarXT for psychosis in schizophrenia, to support and expand company's pipeline of clinical and preclinical programs.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Goldman Sachs & Co. LLC

Deal Size: $460.0 million Upfront Cash: Undisclosed

Deal Type: Public Offering March 24, 2023

blank

08

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : The proceedings will be used to fund Karuna's ongoing and planned clinical trials of KarXT (xanomeline), to support the potential commercialization of KarXT for psychosis in schizophrenia, to support and expand company's pipeline of clinical and preclini...

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : Undisclosed

March 24, 2023

blank

Details:

Under the agreement, Royalty Pharma will acquire PureTech’s royalty in Karuna’s KarXT (xanomeline), an oral, investigational M1/M4-preferring muscarinic agonist for the treatment of psychiatric and neurological conditions, including schizophrenia and psychosis in Alzheimer.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Royalty Pharma

Deal Size: $500.0 million Upfront Cash: $100.0 million

Deal Type: Agreement March 23, 2023

blank

09

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : Under the agreement, Royalty Pharma will acquire PureTech’s royalty in Karuna’s KarXT (xanomeline), an oral, investigational M1/M4-preferring muscarinic agonist for the treatment of psychiatric and neurological conditions, including schizophrenia and...

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : $100.0 million

March 23, 2023

blank

Details:

The proceedings will be used to fund Karuna's ongoing and planned clinical trials of KarXT (xanomeline), to support the potential commercialization of KarXT for psychosis in schizophrenia, to support and expand company's pipeline of clinical and preclinical programs.


Lead Product(s): Xanomeline,Trospium Chloride

Therapeutic Area: Psychiatry/Psychology Brand Name: KarXT

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Goldman Sachs & Co. LLC

Deal Size: $400.0 million Upfront Cash: Undisclosed

Deal Type: Public Offering March 21, 2023

blank

10

ASC 2024
Not Confirmed
ASC 2024
Not Confirmed

Details : The proceedings will be used to fund Karuna's ongoing and planned clinical trials of KarXT (xanomeline), to support the potential commercialization of KarXT for psychosis in schizophrenia, to support and expand company's pipeline of clinical and preclini...

Brand Name : KarXT

Molecule Type : Small molecule

Upfront Cash : Undisclosed

March 21, 2023

blank
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STOCK RECAP #PipelineProspector

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NEWS #PharmaBuzz

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BMS taps Taye Diggs for schizophrenia educational campaign
BMS taps Taye Diggs for schizophrenia educational campaign

22 May 2024

// Andrea Park FIERCE PHARMA

https://www.fiercepharma.com/marketing/bms-taps-taye-diggs-its-best-man-schizophrenia-educational-campaign

Andrea Park FIERCE PHARMA
22 May 2024

https://www.businesswire.com/news/home/20240520903721/en

BUSINESSWIRE
20 May 2024

https://www.biopharmadive.com/news/karuna-schizophrenia-emergent-3-trial-karxt/645392/#:~:text=The%20results%20add%20to%20a,living%20with%20the%20brain%20disorder.&text=An%20experimental%20drug%20from%20Karuna,a%20potential%20therapy%20for%20schizophrenia.

BIOPHARMADIVE
21 Mar 2023

https://www.businesswire.com/news/home/20220822005631/en

BUSINESSWIRE
23 Aug 2022

http://www.pharmafile.com/news/722654/karuna-therapeutics-announces-positive-results-phase-iii-trial-schizophrenia

PHARMA FILE
10 Aug 2022

https://www.businesswire.com/news/home/20220808005231/en

BUSINESS WIRE
08 Aug 2022

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