AMG 319

AMG 319
Clinical data
ATC code	None;
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name (S)-N-(1-[7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl]ethyl)-9H-purin-6-amine;
CAS Number	1608125-21-8 ;
PubChem CID	68947304;
ChemSpider	35000181;
UNII	19DG7G1U5Q;
CompTox Dashboard (EPA)	DTXSID501046373 ;
Chemical and physical data
Formula	C21H16FN7
Molar mass	385.406 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@@H](c1cc2ccc(cc2nc1c3ccccn3)F)Nc4c5c([nH]cn5)ncn4;
	InChI InChI=1S/C21H16FN7/c1-12(28-21-19-20(25-10-24-19)26-11-27-21)15-8-13-5-6-14(22)9-17(13)29-18(15)16-4-2-3-7-23-16/h2-12H,1H3,(H2,24,25,26,27,28)/t12-/m0/s1; Key:KWRYMZHCQIOOEB-LBPRGKRZSA-N;

AMG 319 is a drug developed by Amgen which acts as an inhibitor of the phosphoinositide 3-kinase enzyme subtype PI3Kδ. It was originally developed as an anti-inflammatory drug with potential applications in the treatment of autoimmune conditions such as rheumatoid arthritis, but subsequent research showed that it inhibits cell proliferation and might potentially have useful anti-cancer effects, and it has been put into clinical trials to assess its safety and tolerability in this application.^[1]^[2]

Mechanism(s) of action

It is a potential immunotherapy because blocking PI3Kδ (PI3K p110δ) eliminates a group of inhibitory immune cells and may allow the immune system to better attack the cancer cells.^[3]

Clinical trials

Its first clinical trial was a phase I/II study in adults with relapsed or refractory lymphoid malignancies.^[4] This was due to run from 2011 to 2013.^{[citation needed]}

In 2015/16 it started a phase II clinical trial as a neoadjuvant therapy for human papillomavirus (HPV) negative head and neck squamous-cell carcinoma (HNSCC) (prior to resection surgery).^[3]

References

^ Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, et al. (January 2015). "Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease". Journal of Medicinal Chemistry. 58 (1): 480–511. doi:10.1021/jm501624r. PMID 25469863.
^ Lanasa MC, Glenn MJ, Mato AR, Allgood SD, Wong S, Amore B, et al. (December 2013). First-In-Human Study Of AMG 319, a Highly Selective, Small Molecule Inhibitor Of PI3Kδ, In Adult Patients With Relapsed Or Refractory Lymphoid Malignancies. 55th ASH Annual Meeting and Exposition.
^ ^a ^b Clinical trial number NCT02540928 for "AMG 319 in Human PapillomaVirus (HPV) Negative HNSCC" at ClinicalTrials.gov
^ Clinical trial number NCT01300026 for "A Phase 1, First-in-Human Study Evaluating the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AMG 319 in Adult Subjects With Relapsed or Refractory Lymphoid Malignancies" at ClinicalTrials.gov

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[1] Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, et al. (January 2015). "Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease". Journal of Medicinal Chemistry. 58 (1): 480–511. doi:10.1021/jm501624r. PMID 25469863.

[2] Lanasa MC, Glenn MJ, Mato AR, Allgood SD, Wong S, Amore B, et al. (December 2013). First-In-Human Study Of AMG 319, a Highly Selective, Small Molecule Inhibitor Of PI3Kδ, In Adult Patients With Relapsed Or Refractory Lymphoid Malignancies. 55th ASH Annual Meeting and Exposition.

[NCT02540928-3] Clinical trial number NCT02540928 for "AMG 319 in Human PapillomaVirus (HPV) Negative HNSCC" at ClinicalTrials.gov

[4] Clinical trial number NCT01300026 for "A Phase 1, First-in-Human Study Evaluating the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AMG 319 in Adult Subjects With Relapsed or Refractory Lymphoid Malignancies" at ClinicalTrials.gov

[1]

[2]

[3]

[4]

Mechanism(s) of action

Clinical trials

See also

References