Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM8O3R9)

• Drug Name: APG-1252 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Small-cell lung cancer	2C25.Y	Phase 1/2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 76900653
  TTD Drug ID: DM8O3R9

Molecule-Related Drug Atlas

Drug(s) Targeting Apoptosis regulator Bcl-2 (BCL-2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MCI-186	DM8ZHP1	Amyotrophic lateral sclerosis	8B60.0	Approved	[4]
Taxol	DMUOT9V	Breast cancer	2C60-2C65	Approved	[5]
GDC-0199	DMH0QKA	Chronic lymphocytic leukaemia	2A82.0	Approved	[6]
ABT-263	DMNE56X	Myelofibrosis	2A20.2	Phase 3	[7]
Taxol/Paraplatin/Herceptin	DML6GAN	Breast cancer	2C60-2C65	Phase 3	[8]
Oblimersen	DM7KI4E	Melanoma	2C30	Phase 3	[9]
RG7601	DMDVAFP	Chronic lymphocytic leukaemia	2A82.0	Phase 3	[6]
Thymoquinone	DMVDTR2	Polycystic ovarian syndrome	5A80.1	Phase 2/3	[10]
Obatoclax	DMPF9ZM	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
PI-88/Taxotere	DM4FIWC	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]

Drug(s) Targeting Apoptosis regulator Bcl-xL (BCL-xL)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ABT-263	DMNE56X	Myelofibrosis	2A20.2	Phase 3	[7]
Obatoclax	DMPF9ZM	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
AZD0466	DMWLZI6	Hematologic tumour	2B33.Y	Phase 1/2	[13]
PMID27744724-Compound-18	DM73S2C	N. A.	N. A.	Patented	[14]
Indole-based analog 2	DM0NEVC	N. A.	N. A.	Patented	[14]
PMID27744724-Compound-10	DMFKS2P	N. A.	N. A.	Patented	[14]
PMID27744724-Compound-21	DM18UA5	N. A.	N. A.	Patented	[14]
Indole-based analog 3	DMTEYQJ	N. A.	N. A.	Patented	[14]
PMID27744724-Compound-26	DM8GOH3	N. A.	N. A.	Patented	[14]
PMID27744724-Compound-27	DMV6MLC	N. A.	N. A.	Patented	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Apoptosis regulator Bcl-2 (BCL-2)	TTJGNVC	BCL2_HUMAN	Inhibitor	[3]
Apoptosis regulator Bcl-xL (BCL-xL)	TTU1E82	B2CL1_HUMAN	Inhibitor	[3]

References

• [1] ClinicalTrials.gov (NCT04210037) Study of APG-1252 Plus Paclitaxel in Patients With Relapsed/Refractory Small Cell Lung Cancer. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Bcl-2/Bcl-xl inhibitor APG-1252-M1 is a promising therapeutic strategy for gastric carcinoma. Cancer Med. 2020 Jun;9(12):4197-4206.
• [4] Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
• [5] Paclitaxel directly binds to Bcl-2 and functionally mimics activity of Nur77. Cancer Res. 2009 Sep 1;69(17):6906-14.
• [6] ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8.
• [7] Clinical pipeline report, company report or official report of Roche (2009).
• [8] Two concurrent phase II trials of paclitaxel/carboplatin/trastuzumab (weekly or every-3-week schedule) as first-line therapy in women with HER2-overexpressing metastatic breast cancer: NCCTG study 983252. Clin Breast Cancer. 2005 Dec;6(5):425-32.
• [9] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [10] Apoptosis as a mechanism for the treatment of adult T cell leukemia: promising drugs from benchside to bedside. Drug Discov Today. 2020 Jul;25(7):1189-1197.
• [11] Phase II study of obatoclax mesylate (GX15-070), a small-molecule BCL-2 family antagonist, for patients with myelofibrosis. Clin Lymphoma Myeloma Leuk. 2010 Aug;10(4):285-9.
• [12] Multicentre phase I/II study of PI-88, a heparanase inhibitor in combination with docetaxel in patients with metastatic castrate-resistant prostate cancer. Ann Oncol. 2010 Jun;21(6):1302-7.
• [13] Design and optimisation of dendrimer-conjugated Bcl-2/x L inhibitor, AZD0466, with improved therapeutic index for cancer therapy. Commun Biol. 2021 Jan 25;4(1):112.
• [14] Mcl-1 inhibitors: a patent review.Expert Opin Ther Pat. 2017 Feb;27(2):163-178.