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Chemistry

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Also known as: 1236208-20-0, Leucomethylene blue mesylate, Leucomethylene blue (mesylate), Hydromethylthionine mesylate, N3,n3,n7,n7-tetramethyl-10h-phenothiazine-3,7-diamine dimethanesulfonate, Leucomethylene blue bismesylate
Molecular Formula
C18H27N3O6S3
Molecular Weight
477.6  g/mol
InChI Key
SPCMQFLNOVTUBM-UHFFFAOYSA-N
FDA UNII
3248SEF29D

Hydromethylthionine Mesylate
1 2D Structure

Hydromethylthionine Mesylate

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
methanesulfonic acid;3-N,3-N,7-N,7-N-tetramethyl-10H-phenothiazine-3,7-diamine
2.1.2 InChI
InChI=1S/C16H19N3S.2CH4O3S/c1-18(2)11-5-7-13-15(9-11)20-16-10-12(19(3)4)6-8-14(16)17-13;2*1-5(2,3)4/h5-10,17H,1-4H3;2*1H3,(H,2,3,4)
2.1.3 InChI Key
SPCMQFLNOVTUBM-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CN(C)C1=CC2=C(C=C1)NC3=C(S2)C=C(C=C3)N(C)C.CS(=O)(=O)O.CS(=O)(=O)O
2.2 Other Identifiers
2.2.1 UNII
3248SEF29D
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Hydromethylthionine

2. Hydromethylthionine Mesylate

3. Leuco-methylthioninium

4. Leucomethylene Blue

5. Leukomethylene Blue

6. Lmtx Compound

7. Panatone

8. Trx0237

2.3.2 Depositor-Supplied Synonyms

1. 1236208-20-0

2. Leucomethylene Blue Mesylate

3. Leucomethylene Blue (mesylate)

4. Hydromethylthionine Mesylate

5. N3,n3,n7,n7-tetramethyl-10h-phenothiazine-3,7-diamine Dimethanesulfonate

6. Leucomethylene Blue Bismesylate

7. Lmtm

8. Trx-0237 Dimesylate

9. 3248sef29d

10. Hydromethylthionine Mesylate [usan]

11. Methanesulfonic Acid;3-n,3-n,7-n,7-n-tetramethyl-10h-phenothiazine-3,7-diamine

12. Trx0237

13. Leuco-methylthioninium Dimesylate

14. Trx-0237

15. Lmtx

16. 10h-phenothiazine-3,7-diamine, N3,n3,n7,n7-tetramethyl-, Methanesulfonate (1:2)

17. Trx-0237 Mesylate

18. Trx0237 Dimesylate

19. Trx0237 (lmtx)

20. Unii-3248sef29d

21. Chembl4297221

22. Bcp16840

23. Ex-a1927

24. Mfcd29764308

25. Akos026750731

26. Cs-5553

27. Leucomethylene Blue Mesylate; Trx0237

28. Hy-19948

29. Ms-28864

30. Leucomethylene Blue; Bis(methanesulfonic Acid)

31. A922039

32. Trx0237 Mesylate;methylene Blue Leuco Base Mesylate

33. Leuco-methylthioninium Bis(hydromethanesulfonate)

34. 3,7-bis(dimethylamino)phenothiazin-5-ium Methanesulfonate

35. N3,n3,n7,n7-tetramethyl-10h-phenothiazine-3,7-diaminedimethanesulfonate

36. N,n,n',n'-tetramethyl-10h-phenothiazine-3,7-diaminium Bis(methanesulfonate)

2.3.3 Other Synonyms

1. Hydromethylthionine Mesylate

2.4 Create Date
2012-09-10
3 Chemical and Physical Properties
Molecular Weight 477.6 g/mol
Molecular Formula C18H27N3O6S3
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count10
Rotatable Bond Count2
Exact Mass g/mol
Monoisotopic Mass g/mol
Topological Polar Surface Area169
Heavy Atom Count30
Formal Charge0
Complexity396
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count3

Drugs in Development

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Details:

TRx0237 (hydromethylthionine mesylate), is an investigational small molecule Tau protein inhibitor, for the treatment of mild to moderate Alzheimer’s disease. The company has submitted MAA in UK.


Lead Product(s): Hydromethylthionine Mesylate

Therapeutic Area: Neurology Brand Name: TRx0237

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable July 01, 2024

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01

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

Details : TRx0237 (hydromethylthionine mesylate), is an investigational small molecule Tau protein inhibitor, for the treatment of mild to moderate Alzheimer’s disease. The company has submitted MAA in UK.

Product Name : TRx0237

Product Type : Small molecule

Upfront Cash : Not Applicable

July 01, 2024

blank

Details:

TauRx's lead product candidate TRx0237 (hydromethylthionine), a tau protein inhibitor. Currently, it is being evaluated in the Phase 3 clinical trial studies for the treatment of Alzheimer's disease.


Lead Product(s): Hydromethylthionine Mesylate

Therapeutic Area: Neurology Brand Name: TRx0237

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 07, 2024

blank

02

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

Details : TauRx's lead product candidate TRx0237 (hydromethylthionine), a tau protein inhibitor. Currently, it is being evaluated in the Phase 3 clinical trial studies for the treatment of Alzheimer's disease.

Product Name : TRx0237

Product Type : Small molecule

Upfront Cash : Not Applicable

March 07, 2024

blank

Details:

TRx0237 is a small molecule drug being tested for its ability to inhibit aggregation of tau, a protein that forms neurofibrillary tangles in the brains of people with Alzheimer's and other neurodegenerative diseases.


Lead Product(s): Hydromethylthionine Mesylate

Therapeutic Area: Neurology Brand Name: TRx0237

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 30, 2022

blank

03

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

Details : TRx0237 is a small molecule drug being tested for its ability to inhibit aggregation of tau, a protein that forms neurofibrillary tangles in the brains of people with Alzheimer's and other neurodegenerative diseases.

Product Name : TRx0237

Product Type : Small molecule

Upfront Cash : Not Applicable

November 30, 2022

blank

Details:

HMTM or TRx0237 is an oral tau aggregation inhibitor, targeting this underlying pathology. TauRx’s HMTM has the potential to become the first disease-modifying therapies (DMT) targeting tau to be approved for AD.


Lead Product(s): Hydromethylthionine Mesylate

Therapeutic Area: Neurology Brand Name: TRx0237

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Undisclosed

Deal Size: Undisclosed Upfront Cash: Undisclosed

Deal Type: Financing November 14, 2022

blank

04

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

Details : HMTM or TRx0237 is an oral tau aggregation inhibitor, targeting this underlying pathology. TauRx’s HMTM has the potential to become the first disease-modifying therapies (DMT) targeting tau to be approved for AD.

Product Name : TRx0237

Product Type : Small molecule

Upfront Cash : Undisclosed

November 14, 2022

blank

Details:

For people with early Alzheimer’s (MCI), HMTM, a potent inhibitor of Tau aggregation treatment resulted in sustained improvement in cognition over pre-treatment baseline, and normalisation of brain atrophy to a rate similar to healthy individuals.


Lead Product(s): Hydromethylthionine Mesylate

Therapeutic Area: Neurology Brand Name: TRx0237

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 06, 2022

blank

05

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

Details : For people with early Alzheimer’s (MCI), HMTM, a potent inhibitor of Tau aggregation treatment resulted in sustained improvement in cognition over pre-treatment baseline, and normalisation of brain atrophy to a rate similar to healthy individuals.

Product Name : TRx0237

Product Type : Small molecule

Upfront Cash : Not Applicable

October 06, 2022

blank

Details:

TauRx's lead investigative oral drug, TRx0237, has been tested in 598 people with Alzheimer's. Following our 12 month blinded phase of the study, participants have moved forward to an additional one year open label phase.


Lead Product(s): Hydromethylthionine Mesylate

Therapeutic Area: Neurology Brand Name: TRx0237

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 01, 2022

blank

06

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

Details : TauRx's lead investigative oral drug, TRx0237, has been tested in 598 people with Alzheimer's. Following our 12 month blinded phase of the study, participants have moved forward to an additional one year open label phase.

Product Name : TRx0237

Product Type : Small molecule

Upfront Cash : Not Applicable

June 01, 2022

blank

Details:

This milestone means TauRx will now progress to the data cleaning and analysis phase which enables the company to determine topline results on the safety and efficacy of Hydromethylthionine mesylate (HMTM).


Lead Product(s): Hydromethylthionine Mesylate

Therapeutic Area: Neurology Brand Name: TRx0237

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable April 14, 2022

blank

07

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

Details : This milestone means TauRx will now progress to the data cleaning and analysis phase which enables the company to determine topline results on the safety and efficacy of Hydromethylthionine mesylate (HMTM).

Product Name : TRx0237

Product Type : Small molecule

Upfront Cash : Not Applicable

April 14, 2022

blank

Details:

Minimum dose of hydromethylthionine could slow clinical decline and brain atrophy in behavioural variant Fronto-Temporal Dementia as well as Alzheimer's Disease.


Lead Product(s): Hydromethylthionine Mesylate

Therapeutic Area: Neurology Brand Name: TRx0237

Study Phase: Phase IIIProduct Type: Small molecule

Sponsor: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 19, 2020

blank

08

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

TauRx Therapeutics

Singapore
arrow
Biotech Digital Meet
Not Confirmed

Details : Minimum dose of hydromethylthionine could slow clinical decline and brain atrophy in behavioural variant Fronto-Temporal Dementia as well as Alzheimer's Disease.

Product Name : TRx0237

Product Type : Small molecule

Upfront Cash : Not Applicable

May 19, 2020

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