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13 Listed Suppliers
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18 US Patents
6 US Exclusivities

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Ozanimod Hydrochloride

Synopsis

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Chemistry

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Also known as: 1306760-87-1, Rpc1063, Rpc-1063, Ozanimod (rpc1063), (s)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1h-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile, Z80293urpv

Molecular Formula

C₂₃H₂₄N₄O₃

Molecular Weight

404.5 g/mol

InChI Key

XRVDGNKRPOAQTN-FQEVSTJZSA-N

FDA UNII

Z80293URPV

Ozanimod is an orally bioavailable sphingosine-1-phosphate (S1P) receptors 1 (S1PR1, S1P1) and 5 (S1PR5, S1P5) modulator, with potential anti-inflammatory and immunomodulating activities. Upon oral administration, ozanimod selectively targets and binds to S1PR1 on lymphocytes and induces S1PR1 internalization and degradation. This results in the sequestration of lymphocytes in lymph nodes. By preventing egress of lymphocytes, ozanimod reduces both the amount of circulating peripheral lymphocytes and the infiltration of lymphocytes into target tissues. This prevents a lymphocyte-mediated immune response and may reduce inflammation. S1PR1, a G-protein coupled receptor, plays a key role in lymphocyte migration from lymphoid tissues. Modulation of S1PR5 by ozanimod may be neuroprotective.

1 2D Structure

Ozanimod Hydrochloride

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

5-[3-[(1S)-1-(2-hydroxyethylamino)-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile

2.1.2 InChI

InChI=1S/C23H24N4O3/c1-14(2)29-21-9-6-15(12-16(21)13-24)23-26-22(27-30-23)19-5-3-4-18-17(19)7-8-20(18)25-10-11-28/h3-6,9,12,14,20,25,28H,7-8,10-11H2,1-2H3/t20-/m0/s1

2.1.3 InChI Key

XRVDGNKRPOAQTN-FQEVSTJZSA-N

2.1.4 Canonical SMILES

CC(C)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CCC(C4=CC=C3)NCCO)C#N

2.1.5 Isomeric SMILES

CC(C)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CC[C@@H](C4=CC=C3)NCCO)C#N

2.2 Other Identifiers

2.2.1 UNII

Z80293URPV

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Rpc1063

2.3.2 Depositor-Supplied Synonyms

1. 1306760-87-1

2. Rpc1063

3. Rpc-1063

4. Ozanimod (rpc1063)

5. (s)-5-(3-(1-((2-hydroxyethyl)amino)-2,3-dihydro-1h-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-isopropoxybenzonitrile

6. Z80293urpv

7. Zeposia

8. Unii-z80293urpv

9. Benzonitrile, 5-(3-((1s)-2,3-dihydro-1-((2-hydroxyethyl)amino)-1h-inden-4-yl)-1,2,4-oxadiazol-5-yl)-2-(1-methylethoxy)-

10. Ozanimod [inn]

11. 5-[3-[(1~{s})-1-(2-hydroxyethylamino)-2,3-dihydro-1~{h}-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxy-benzenecarbonitrile

12. Benzonitrile, 5-[3-[(1s)-2,3-dihydro-1-[(2-hydroxyethyl)amino]-1h-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)-

13. Ozanimod [usan:inn]

14. 5-[3-[(1s)-1-(2-hydroxyethylamino)-2,3-dihydro-1h-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile

15. Rpc 1063

16. Ozanimod [usan]

17. Ozanimod; Rpc1063

18. Ozanimod (usan/inn)

19. Ozanimod [mi]

20. Ozanimod [who-dd]

21. Gtpl8709

22. Schembl2195490

23. Chembl3707247

24. Amy3373

25. Dtxsid501026488

26. Bcp16513

27. Ex-a1316

28. Rpc1063:rpc-1063

29. Bdbm50507186

30. Mfcd28386168

31. S7952

32. Akos026674086

33. Zinc116109867

34. Ccg-268695

35. Cs-5070

36. Db12612

37. Ac-29883

38. As-75063

39. Hy-12288

40. J3.612.016i

41. D10968

42. P14657

43. Q21098986

44. 5-{3-[(1s)-1-[(2-hydroxyethyl)amino]-2,3-dihydro-1h-inden-4-yl]-1,2,4-oxadiazol-5-yl}-2-(propan-2-yloxy)benzonitrile

45. Jeu

2.4 Create Date

2011-06-13

3 Chemical and Physical Properties

Molecular Formula	C₂₃H₂₄N₄O₃
Molecular Weight	404.5 g/mol
XLogP3	3.1
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	7
Exact Mass	404.18484064 g/mol
Monoisotopic Mass	404.18484064 g/mol
Topological Polar Surface Area	104 Å²
Heavy Atom Count	30
Formal Charge	0
Complexity	609
Isotope Atom Count	0
Defined Atom Stereocenter Count	1
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

Ozanimod is indicated for adults in the treatment of relapsing forms of MS, which may include relapsing-remitting disease, clinically isolated syndrome, and active secondary progressive MS.

FDA Label

Multiple sclerosis

- Zeposia is indicated for the treatment of adult patients with relapsing remitting multiple sclerosis (RRMS) with active disease as defined by clinical or imaging features.

Ulcerative colitis

- Zeposia is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis (UC) who have had an inadequate response, lost response, or were intolerant to either conventional therapy or a biologic agent.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Ozanimod reduces circulating lymphocytes that cause the neuroinflammation associated with MS, reducing debilitating symptoms and, possibly, disease progression. During clinical trials, ozanimod reduced MS-associated brain volume loss in several regions. Ozanimod causes the sequestration of peripheral lymphocytes, reducing circulating lymphocytes in the gastrointestinal tract.

5.2 MeSH Pharmacological Classification

Sphingosine 1 Phosphate Receptor Modulators

Agents that affect the function of G-protein coupled SPHINGOSINE 1-PHOSPHATE RECEPTORS. Their binding to the receptors blocks lymphocyte migration and are often used as IMMUNOSUPPRESSANTS. (See all compounds classified as Sphingosine 1 Phosphate Receptor Modulators.)

5.3 ATC Code

L04AA38

L - Antineoplastic and immunomodulating agents

L04 - Immunosuppressants

L04A - Immunosuppressants

L04AA - Selective immunosuppressants

L04AA38 - Ozanimod

5.4 Absorption, Distribution and Excretion

Absorption

Ozanimod is absorbed in the gastrointestinal tract after oral administration. The Cmax of ozanimod is 0.244 ng/mL and is achieved at 6 to 8 hours after administration, reaching steady-state at about 102 hours after administration. The AUC is 4.46 ng*h/mL. Its delayed absorption reduces effects that may occur after the first dose, such as heart rate changes. The peak plasma concentration of ozanimod is low due to a high volume of distribution.

Route of Elimination

The kidneys are not a major source of elimination for ozanimod. After a 0.92 mg dose of radiolabeled ozanimod was administered, about 26% of the labeled drug was accounted for in the urine and 37 % in the feces, mainly in the form of inactive metabolites.

Volume of Distribution

The average volume of distribution of ozanimod is 5590L. Another reference mentions a volume of distribution ranging from 73-101 L/kg. This drug crosses the blood-brain barrier.

Clearance

The mean apparent oral clearance of ozanimod, according to prescribing information, is 192 L/h. Another reference indicates an oral clearance of 233 L/h.

5.5 Metabolism/Metabolites

Ozanimod has two major active metabolites CC112273 and CC1084037 and minor active metabolites such as RP101988, RP101075, and RP101509, which target the S1P1 and S1P5 receptors. The enzymes involved in the metabolism of ozanimod include ALDH/ADH, NAT-2, Monoamine Oxidase B, and AKR 1C1/1C2. After metabolism, ozanimod (6%), CC112273 (73%), and CC1084037 (15%) are accounted for in the circulation.

5.6 Biological Half-Life

The half-life of ozanimod ranges from 17-21 hours.

5.7 Mechanism of Action

Sphingosine1phosphate (S1P) is an important phospholipid that binds to various Gproteincoupled receptor subtypes, which can be identified as S1P15R. S1P and the receptors it binds to perform regular functions in the immune, cardiovascular, pulmonary, and nervous system. S1P can be expressed ubiquitously, playing an important role in regulating inflammation. S1P1R, S1P2R, and S1P3R receptors can be found in the cardiovascular, immune, and central nervous systems. S1P4R is found on lymphocytic and hematopoietic cells, while S1P5R expression is found only on the spleen (on natural killer cells) or in the central nervous system. Ozanimod is a selective modulator of S1P receptors and binds to S1P1R and S1P5R subtypes. The mechanism of action of ozanimod is not fully understood, but this drug likely reduces the migration of lymphocytes that usually aggravate the inflammation associated with MS.

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