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9 Drugs in Development

9 Drugs in Development

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Also known as: Cpi-0610, 1380087-89-7, Cpi 0610, (s)-2-(6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, Chembl4303404, Cpi-232

Molecular Formula

C₂₀H₁₆ClN₃O₂

Molecular Weight

365.8 g/mol

InChI Key

GCWIQUVXWZWCLE-INIZCTEOSA-N

FDA UNII

U4017GUQ06

Pelabresib Anhydrous is the anhydrous form of pelabresib, a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon administration, pelabresib binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of two bromodomains at the N-terminus, the BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that play an important role during development and cellular growth.

1 2D Structure

Pelabresib

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

2-[(4S)-6-(4-chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide

2.1.2 InChI

InChI=1S/C20H16ClN3O2/c1-11-18-14-4-2-3-5-15(14)19(12-6-8-13(21)9-7-12)23-16(10-17(22)25)20(18)26-24-11/h2-9,16H,10H2,1H3,(H2,22,25)/t16-/m0/s1

2.1.3 InChI Key

GCWIQUVXWZWCLE-INIZCTEOSA-N

2.1.4 Canonical SMILES

CC1=NOC2=C1C3=CC=CC=C3C(=NC2CC(=O)N)C4=CC=C(C=C4)Cl

2.1.5 Isomeric SMILES

CC1=NOC2=C1C3=CC=CC=C3C(=N[C@H]2CC(=O)N)C4=CC=C(C=C4)Cl

2.2 Other Identifiers

2.2.1 UNII

U4017GUQ06

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Cpi-0610

2.3.2 Depositor-Supplied Synonyms

1. Cpi-0610

2. 1380087-89-7

3. Cpi 0610

4. (s)-2-(6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide

5. Chembl4303404

6. Cpi-232

7. U4017guq06

8. Pelabresib

9. Cpi-267232

10. 2-[(4s)-6-(4-chlorophenyl)-1-methyl-4h-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide

11. Cpi0610

12. 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-isoxazolo(5,4-d)(2)benzazepin-4-yl)acetamide

13. 4h-isoxazolo(5,4-d)(2)benzazepine-4-acetamide, 6-(4-chlorophenyl)-1-methyl-, (4s)

14. Pelabresib [inn]

15. Pelabresib Anhydrous

16. Unii-u4017guq06

17. Gtpl9120

18. Schembl15926539

19. Dtxsid201022544

20. Bcp10741

21. Ex-a1612

22. Bdbm50510872

23. Nsc784856

24. S7853

25. Akos030526467

26. Zinc200480149

27. Cs-5592

28. Nsc-784856

29. Compound 10 [pmid: 26815195]

30. Ncgc00483135-01

31. As-73876

32. Bc177446

33. Hy-12863

34. J3.554.939k

35. Q27076907

36. 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide

37. 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[e]isoxazolo[5,4-c]azepin-4-yl)acetamide

38. 2-[(7s)-9-(4-chlorophenyl)-3-methyl-5-oxa-4,8-diazatricyclo[8.4.0.0(2),?]tetradeca-1(10),2(6),3,8,11,13-hexaen-7-yl]acetamide

39. 62g

2.4 Create Date

2012-07-23

3 Chemical and Physical Properties

Molecular Formula	C₂₀H₁₆ClN₃O₂
Molecular Weight	365.8 g/mol
XLogP3	3
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Exact Mass	365.0931045 g/mol
Monoisotopic Mass	365.0931045 g/mol
Topological Polar Surface Area	81.5 Å²
Heavy Atom Count	26
Formal Charge	0
Complexity	561
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

Drugs in Development

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Pipeline Prospector Feb 2024: Novo’s parent buys Catalent for US$ 16.5 bn, FDA okays Iovance’s cell therapy

February was a good month for the pharma sector, complete with some important deals, successes from clinical trials and healthy fourth quarter (Q4) results announced by some drugmakers. The market cheered the good news — the Nasdaq Biotechnology index gained 1 percent from 4,385.06 to 4,428.56, the SPDR S&P Biotech ETF index spiked 12 percent to 98.42 after ending January at 87.43. The S&P Biotechnology Select Industry Index (SPSIBI) soared 16 percent from 6,815.3 to 7,896.47 in February.The month saw some big acquisitions. Novo Holdings, the parent company of Novo Nordisk, acquired contract development and manufacturing organization (CDMO) Catalent for US$ 16.5 billion. Novo Holdings plans to sell three of Catalent’s “fill-finish” sites to Novo Nordisk for US$ 11 billion. Novo’s game plan hasn’t gone down well with its arch rival in the diabetes and obesity segment Eli Lilly. The Indianapolis-headquartered drugmaker has called for a scrutiny of the deal as it relies on Catalent for some of its diabetes and obesity drugs that compete with Novo’s meds.Both Novo and Lilly have been struggling to meet the demand for their weight loss meds. With the acquisition of this key CDMO, Novo has scored an edge over competition.Meanwhile, Gilead boosted its liver portfolio with the US$ 4.3 billion acquisition of CymaBay Therapeutics. And Novartis announced the acquisition of cancer treatment developer MorphoSys for € 2.7 billion (US$ 2.9 billion). With this buyout, Novartis gets a late-stage, rare bone-marrow cancer treatment — pelabresib — that holds plenty of promise.Several drugmakers announced their Q4 results last month. Notable amongst them was Eli Lilly, as it posted a 28 percent increase in revenues — from US$ 7.3 billion in Q4 2022 to US$ 9.4 billion led by its new products Mounjaro and Zepbound. GSK touted the “exceptional launch of Arexvy”, the world's first RSV vaccine, as it brought in sales of £ 1.2 billion (US$ 1.52 billion) in 2023. And Merck’s Keytruda saw a 19 percent increase in its sales in 2023 — at US$ 25 billion.Access the Pipeline Prospector Dashboard for February 2024 Newsmakers (Free Excel)FDA okays Iovance’s T-cell therapy; Roche’s asthma med okayed for food allergiesThe US Food and Drug Administration (FDA) granted accelerated approval to Iovance Biotherapeutics’ cell therapy — Amtagvi (lifileucel) — for treating the deadliest form of skin cancer. Amtagvi is the first and only one-time, individualized T cell therapy to receive FDA approval for a solid tumor cancer. Iovance hopes to start reporting noteworthy revenue in the second quarter of 2024, despite the fact that Amtagvi comes with a boxed warning (the highest safety warning) for treatment-related mortality. FDA also approved Takeda’s Eohilia as the first oral treatment for an allergic inflammation of the esophagus. Eohilia (budesonide oral suspension) was on course to becoming the first treatment for eosinophilic esophagitis (EoE) until it was rejected by the FDA in December 2021.In January, Sanofi and Regeneron’s jab Dupixent had pipped Eohilia to become the first FDA drug approved for EoE. The chronic condition can make it very hard for patients to consume food. Dupixent (dupilumab) is injected weekly or biweekly and two pens cost US$ 3,803.20. In contrast, Takeda’s drug is taken twice daily and costs US$ 1,875 per month.Roche and Novartis’ asthma drug Xolair (omalizumab) became the first FDA-approved med to help people with food allergies avoid severe reactions following accidental exposure. This opens the drug to around 17 million people in the US whose allergies can potentially be deadly.Access the Pipeline Prospector Dashboard for February 2024 Newsmakers (Free Excel) Boehringer’s obesity candidate, Lilly’s tirzepatide show promise in trials for MASHBoehringer Ingelheim announced promising phase 2 trial data for its experimental obesity drug survodutide in treating metabolic dysfunction-associated steatohepatitis (MASH), a liver disease. The drug is being developed in collaboration with Zealand Pharma. It had received a fast-track designation from the FDA in June 2021. MASH causes histologic liver damage and occurs in patients who are not alcoholics and who are often obese or have type 2 diabetes.The trial met its primary endpoint with survodutide reaching a biopsy-proven improvement in MASH after 48 weeks. Survodutide also met all secondary endpoints, including a statistically significant improvement in liver fibrosis. The companies said this potentially positions it as a “best-in-class” treatment. The drug belongs to the glucagon-like peptide 1 (GLP-1) class of drugs.In another trial, Eli Lilly announced positive results from a phase 2 study of tirzepatide in adults with MASH — 74 percent of participants were cured of MASH and their fibrosis also did not worsen at 52 weeks (as compared to nearly 13 percent for participants in the placebo group).Access the Pipeline Prospector Dashboard for February 2024 Newsmakers (Free Excel) J&J’s autoimmune drug posts trial gains; Sanofi’s frexalimab shows benefit in MSOne of Johnson & Johnson’s most watched experimental drugs — nipocalimab — posted positive results in trials for the treatment of two autoimmune disorders. In a phase 3 study, nipocalimab significantly reduced symptoms of generalized myasthenia gravis (GMG). And, in a phase 2 study, it helped reduce the severity of Sjögren’s disease (SjD). GMG weakens the skeletal muscles and particularly affects control of the limbs, throat, mouth, and eyes. SjD is an immune disorder that is identified by symptoms like dry eyes and dry mouth. J&J expects over US$ 5 billion from this drug. In a phase 2 trial, Sanofi’s frexalimab significantly slowed disease activity in people with relapsing multiple sclerosis (MS). In December last year, the French multinational had named frexalimab as one of three “pipeline-in-a-product” assets with the potential of generating annual peak sales in excess of €5 billion (US$ 5.4 billion). The phase 2 results give credence to those expectations.In trial failures, Gilead (stock down 8 percent) said the FDA has paused all trials of its drug magrolimab in the treatment of two blood cancers – acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) – because of increased risk of patient death (when used in combination with azacitidine plus venetoclax). Magrolimab was the lead candidate of Gilead’s US$ 4.9 billion acquisition of Forty Seven in 2020.Access the Pipeline Prospector Dashboard for February 2024 Newsmakers (Free Excel) Our viewThe year has gotten off to a good start with drugmakers posting healthy Q4 results and the indices showing some positive growth month-on-month. Several drugmakers have entered 2024 with a simplified business model and an increased strategic focus on R&D. Given the favorable demand, we are hopeful of a better year for the industry, as opposed to the volatility of the last two years.Access the Pipeline Prospector Dashboard for February 2024 Newsmakers (Free Excel)

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