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1. Supplementary Materials, Figure Legends 1-6 from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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2. Data from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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3. Supplementary Figure 5 from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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4. Supplementary Tables 1-3 from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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5. Supplementary Figure 3 from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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6. Supplementary Figure 1 D-H from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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7. Supplementary Figure 1 A-C from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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8. Supplementary Figure 6 from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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9. Supplementary Figure 4 from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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10. Supplementary Figure 2 from R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, primary, Franci, Christian, primary, Hu, Yuanming, primary, Chang, Betty, primary, Li, Weiqun, primary, Duan, Matt, primary, Torneros, Allan, primary, Yu, Jiaxin, primary, Heckrodt, Thilo J., primary, Zhang, Jing, primary, Ding, Pingyu, primary, Apatira, Ayodele, primary, Chua, Joanne, primary, Brandt, Ralf, primary, Pine, Polly, primary, Goff, Dane, primary, Singh, Rajinder, primary, Payan, Donald G., primary, and Hitoshi, Yasumichi, primary

Published
2023
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11. R723, a selective JAK2 inhibitor, effectively treats JAK2V617F-induced murine myeloproliferative neoplasm

Author

Shide, Kotaro, Kameda, Takuro, Markovtsov, Vadim, Shimoda, Haruko K., Tonkin, Elizabeth, Fang, Shuling, Liu, Chian, Gelman, Marina, Lang, Wayne, Romero, Jason, McLaughlin, John, Bhamidipati, Somasekhar, Clough, Jeffrey, Low, Caroline, Reitsma, Andrea, Siu, Stacey, Pine, Polly, Park, Gary, Torneros, Allan, Duan, Matt, Singh, Rajinder, Payan, Donald G., Matsunaga, Takuya, Hitoshi, Yasumichi, and Shimoda, Kazuya

Published
2011
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13. R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer

Author

Holland, Sacha J., primary, Pan, Alison, additional, Franci, Christian, additional, Hu, Yuanming, additional, Chang, Betty, additional, Li, Weiqun, additional, Duan, Matt, additional, Torneros, Allan, additional, Yu, Jiaxin, additional, Heckrodt, Thilo J., additional, Zhang, Jing, additional, Ding, Pingyu, additional, Apatira, Ayodele, additional, Chua, Joanne, additional, Brandt, Ralf, additional, Pine, Polly, additional, Goff, Dane, additional, Singh, Rajinder, additional, Payan, Donald G., additional, and Hitoshi, Yasumichi, additional

Published
2010
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14. Efficacy of R723, a Potent and Selective JAK2 Inhibitor, in JAK2V617F-Induced Murine MPD Model.

Author

Shide, Kotaro, primary, Kameda, Takuro, additional, Markovtsov, Vadim, additional, Matsunaga, Takuya, additional, Shimoda, Haruko, additional, Hidaka, Tomonori, additional, Katayose, Keiko, additional, Kubuki, Yoko, additional, Bhamidipati, Somasekhar, additional, Park, Gary, additional, Torneros, Allan, additional, Duan, Matt, additional, Hitoshi, Yasumichi, additional, and Shimoda, Kazuya, additional

Published
2009
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15. In Vitro and in Vivo Inhibition of JAK2 Signaling by Potent and Selective JAK2 Inhibitor

Author

Markovtsov, Vadim, primary, Tonkin, Elizabeth, additional, Fang, Shuling, additional, Liu, Chiang, additional, Gelman, Marina, additional, Lang, Wayne, additional, Romero, Jason, additional, McLaughlin, John, additional, Bhamidipati, Somasekhar, additional, Clough, Jeffrey, additional, Singh, Rajinder, additional, Low, Caroline, additional, Reitsma, Andrea, additional, Taylor, Vanessa, additional, Siu, Stacey, additional, Park, Gary, additional, Sweeney, David, additional, Pine, Polly, additional, Torneros, Allan, additional, Clemens, George, additional, Duan, Matt, additional, Daniel, Ruby, additional, Payan, Donald, additional, Holland, Sacha, additional, and Hitoshi, Yasumichi, additional

Published
2008
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16. XP13512 [(±)-1-([(α-Isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane Acetic Acid], A Novel Gabapentin Prodrug: II. Improved Oral Bioavailability, Dose Proportionality, and Colonic Absorption Compared with Gabapentin in Rats and Monkeys

Author

Cundy, Kenneth C., primary, Annamalai, Thamil, additional, Bu, Lin, additional, De Vera, Josephine, additional, Estrela, Jenny, additional, Luo, Wendy, additional, Shirsat, Payal, additional, Torneros, Allan, additional, Yao, Fenmei, additional, Zou, Joan, additional, Barrett, Ronald W., additional, and Gallop, Mark A., additional

Published
2004
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17. XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys.

Author

Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, and Gallop MA

Subjects
Administration, Oral, Amines cerebrospinal fluid, Animals, Biological Availability, Carbamates cerebrospinal fluid, Cyclohexanecarboxylic Acids cerebrospinal fluid, Gabapentin, Haplorhini, Injections, Intravenous, Intestinal Absorption physiology, Rats, Rats, Sprague-Dawley, Species Specificity, Tissue Distribution, gamma-Aminobutyric Acid cerebrospinal fluid, Amines pharmacokinetics, Carbamates pharmacokinetics, Colon metabolism, Cyclohexanecarboxylic Acids pharmacokinetics, Prodrugs metabolism, gamma-Aminobutyric Acid analogs & derivatives, gamma-Aminobutyric Acid pharmacokinetics
Abstract

The absorption of gabapentin (Neurontin) is dose-dependent and variable between patients. Rapid clearance of the drug necessitates dosing three or more times per day to maintain therapeutic levels. These deficiencies appear to result from the low capacity, limited intestinal distribution, and variable expression of the solute transporter responsible for gabapentin absorption. Saturation of this transporter at doses used clinically leads to unpredictable drug exposure and potentially ineffective therapy in some patients. XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl]aminomethyl)-1-cyclohexane acetic acid] is a novel prodrug of gabapentin designed to be absorbed by high-capacity nutrient transporters located throughout the intestine. XP13512 was efficiently absorbed and rapidly converted to gabapentin after oral dosing in rats and monkeys. Exposure to gabapentin was proportional to prodrug dose, whereas exposure to intact XP13512 was low. In rats, >95% of an oral dose of (14)C-XP13512 was excreted in urine in 24 h as gabapentin. In monkeys, oral bioavailability of gabapentin from XP13512 capsules was 84.2% compared with 25.4% after a similar oral Neurontin dose. Compared with intracolonic gabapentin, intracolonic XP13512 gave a 17-fold higher gabapentin exposure in rats and 34-fold higher in monkeys. XP13512 may therefore be incorporated into a sustained release formulation to provide extended gabapentin exposure. XP13512 demonstrated improved gabapentin bioavailability, increased dose proportionality, and enhanced colonic absorption. In clinical use, XP13512 may improve the treatment of neuropathic pain, epilepsy, and numerous other conditions by increasing efficacy, reducing interpatient variability, and decreasing frequency of dosing.

Published
2004
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