Details of the Drug Combinations

General Information of This Drug (ID: DMBL3VD)

• Drug Name: PF-05212384 (DMBL3VD)
• Synonyms: PKI-587; 1197160-78-3; Gedatolisib; PF-05212384; PKI587; PKI 587; 1-(4-(4-(Dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea; PF 05212384; UNII-96265TNH2R; PF-05212384 (PKI-587); CHEMBL592445; 96265TNH2R; N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea; Gedatolisib (PF-05212384, PKI-587); Urea, N-(4-((4-(dimethylamino)-1-piperidinyl)carbonyl)phenyl)-N'-(4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl)-

Indication

Solid tumour/cancer; ICD 11: 2A00-2F9Z; Status: Phase 2 [1]

• Drug Type: Small molecular drug

List of Combinatorial Drugs (CBD) Containing This Drug

4 Investigative Drug Combination(s) Consisting of This drug

Normalized Drug Combination Synergy Score

Synergy scores were normalized using Min-Max Scaling to facilitate visual comparisons.

DrugCom Name	DrugCom ID	Component Drug	Indication	REF
PF-05212384 + Ruxolitinib	DCU5B0S	Ruxolitinib	T-cell leukemia/lymphoma (Cell Line: ED-40515)	[2]
PF-05212384 + LY335979	DCLOVFH	LY335979	Human papillomavirus-related cervical adenocarcinoma (Cell Line: KB-ChR-8-5-11)	[2]
PF-05212384 + Panobinostat	DCNMPL4	Panobinostat	Diffuse intrinsic pontine glioma (Cell Line: DIPG25)	[2]
PF-05212384 + Elacridar	DCYHZBK	Elacridar	Human papillomavirus-related cervical adenocarcinoma (Cell Line: KB-ChR-8-5-11)	[2]

10 Clinical Trial Drug Combination(s) Consisting of This drug

DrugCom Name	DrugCom ID	Component Drug	Indication	REF
PD-0325901 + PF-05212384	DCHCXN7	PD-0325901	Advanced Cancer	[3]
PF-05212384 + Irinotecan	DC8VT9R	Irinotecan	Advanced Cancer	[3]
PF-05212384 + Dacomitinib	DC8U0J7	Dacomitinib	Neoplasm	[4]
PF-05212384 + Darolutamide	DCAEQ4W	Darolutamide	MCRPC (Metastatic Castration-resistant Prostate Cancer)	[5]
PF-05212384 + Docetaxel	DCKJ6WF	Docetaxel	Neoplasm	[4]
PF-05212384 + Hydroxychloroquine	DCNISK7	Hydroxychloroquine	Breast Cancer	[6]
PF-05212384 + Palbociclib	DCPDJND	Palbociclib	Lung Cancer Squamous Cell	[7]
Talazoparib + PF-05212384	DCXWFUO	Talazoparib	TNBC - Triple-Negative Breast Cancer	[8]
Fulvestrant + PF-05212384	DCDKVGD	Fulvestrant	Breast Cancer	[9]
Fulvestrant + PF-05212384	DCG6UGG	Fulvestrant	Breast Cancer	[9]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7940).
• [2] Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
• [3] ClinicalTrials.gov (NCT01347866) Clinical Study Of PI3K/mTOR Inhibitors In Combination With An Oral MEK Inhibitor Or Irinotecan In Patients With Advanced Cancer
• [4] ClinicalTrials.gov (NCT01920061) A Study Of PF-05212384 In Combination With Other Anti-Tumor Agents and in Combination With Cisplatin in Patients With Triple Negative Breast Cancer in an Expansion Arm (TNBC)
• [5] ClinicalTrials.gov (NCT06190899) Gedatolisib in Combination With Darolutamide in Metastatic Castration-Resistant Prostate Cancer
• [6] ClinicalTrials.gov (NCT03400254) Gedatolisib, Hydroxychloroquine or the Combination for Prevention of Recurrent Breast Cancer ("GLACIER")
• [7] ClinicalTrials.gov (NCT03065062) Study of the CDK4/6 Inhibitor Palbociclib (PD-0332991) in Combination With the PI3K/mTOR Inhibitor Gedatolisib (PF-05212384) for Patients With Advanced Squamous Cell Lung, Pancreatic, Head & Neck and Other Solid Tumors
• [8] ClinicalTrials.gov (NCT03911973) Gedatolisib Plus Talazoparib in Advanced Triple Negative or BRCA1/2 Positive, HER2 Negative Breast Cancers
• [9] ClinicalTrials.gov (NCT05501886) Gedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1)