AMG319

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 Y

PubChem CID|

* 68947304

ChemSpider|

* 35000181

Chemical and physical data
Formula| C21H16FN7
Molar mass| 385.396 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

AMG319 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]

## Contents

* 1 Mechanism(s) of action
* 2 Clinical trials
* 3 See also
* 4 References

## 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] p110δ inactivation in regulatory T cells unleashes CD8+ cytotoxic T cells.[4]

## Clinical trials

Its first clinical trial was a phase I/II study in adults with relapsed or refractory lymphoid malignancies.[5] This was due to run from 2011 to 2013.

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]

## See also

* Duvelisib
* Idelalisib

## References

1. ↑ Cushing, TD; Hao, X; Shin, Y; Andrews, K; Brown, M; Cardozo, M; Chen, Y; Duquette, J et al. (8 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, Means GD, Stevens E, Yan C, Friberg G, Goy A. 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, December 2013
3. ↑ 3.0 3.1 AMG 319 in Human PapillomaVirus (HPV) Negative HNSCC
4. ↑ Ali, Khaled; Soond, Dalya R.; Piñeiro, Roberto; Hagemann, Thorsten; Pearce, Wayne; Lim, Ee Lyn; Bouabe, Hicham; Scudamore, Cheryl L. et al. (2014). "Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer". Nature 510 (7505): 407–11. doi:10.1038/nature13444. PMID 24919154.
5. ↑ 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

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*[CID]: Compound ID